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1.
Molecules ; 22(11)2017 Nov 07.
Artigo em Inglês | MEDLINE | ID: mdl-29112162

RESUMO

Candidiasis represent a serious threat for patients with altered immune responses. Therefore, we have undertaken the synthesis of compounds comprising a pyridine-3-sulfonamide scaffold and known antifungally active 1,2,4-triazole substituents. Thus a series of novel 4-substituted N-(5-amino-1H-1,2,4-triazol-3-yl)pyridine-3-sulfonamides have been synthesized by multistep reactions starting from 4-chloropyridine-3-sulfonamide via N'-cyano-N-[(4-substitutedpyridin-3-yl)sulfonyl]carbamimidothioates which were further converted with hydrazine hydrate to the corresponding 1,2,4-triazole derivatives 26-36. The final compounds were evaluated for antifungal activity against strains of the genera Candida, Geotrichum, Rhodotorula, and Saccharomycess isolated from patients with mycosis. Many of them show greater efficacy than fluconazole, mostly towards Candida albicans and Rhodotorula mucilaginosa species, with MIC values ≤ 25 µg/mL. A docking study of the most active compounds 26, 34 and 35 was performed showing the potential mode of binding to Candida albicans lanosterol 14α-demethylase. Also in vitro cytotoxicity of selected compounds have been evaluated on the NCI-60 cell line panel.


Assuntos
Antifúngicos/síntese química , Antifúngicos/farmacologia , Sulfonamidas/síntese química , Sulfonamidas/farmacologia , Antifúngicos/química , Candida/efeitos dos fármacos , Desenho de Fármacos , Geotrichum/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Micoses/microbiologia , Rhodotorula/efeitos dos fármacos , Relação Estrutura-Atividade , Sulfonamidas/química
2.
Int J Med Sci ; 13(10): 772-782, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27766027

RESUMO

Objectives: In dentistry, silver nanoparticles (AgNPs) have drawn particular attention because of their wide antimicrobial activity spectrum. However, controversial information on AgNPs toxicity limited their use in oral infections. Therefore, the aim of the present study was to evaluate the antibacterial activities against a panel of oral pathogenic bacteria and bacterial biofilms together with potential cytotoxic effects on human gingival fibroblasts of 10 nm AgNPs: non-functionalized - uncapped (AgNPs-UC) as well as surface-functionalized with capping agent: lipoic acid (AgNPs-LA), polyethylene glycol (AgNPs-PEG) or tannic acid (AgNPs-TA) using silver nitrate (AgNO3) as control. Methods: The interaction of AgNPs with human gingival fibroblast cells (HGF-1) was evaluated using the mitochondrial metabolic potential assay (MTT). Antimicrobial activity of AgNPs was tested against anaerobic Gram-positive and Gram-negative bacteria isolated from patients with oral cavity and respiratory tract infections, and selected aerobic Staphylococci strains. Minimal inhibitory concentration (MIC) values were determined by the agar dilution method for anaerobic bacteria or broth microdilution method for reference Staphylococci strains and Streptococcus mutans. These strains were also used for antibiofilm activity of AgNPs. Results: The highest antimicrobial activities at nontoxic concentrations were observed for the uncapped AgNPs and the AgNPs capped with LA. It was found that AgNPs-LA and AgNPs-PEG demonstrated lower cytotoxicity as compared with the AgNPs-TA or AgNPs-UC in the gingival fibroblast model. All of the tested nanoparticles proved less toxic and demonstrated wider spectrum of antimicrobial activities than AgNO3 solution. Additionally, AgNPs-LA eradicated Staphylococcus epidermidis and Streptococcus mutans 1-day biofilm at concentration nontoxic to oral cells. Conclusions: Our results proved that a capping agent had significant influence on the antibacterial, antibiofilm activity and cytotoxicity of AgNPs. Clinical significance: This study highlighted potential usefulness of AgNPs against oral anaerobic Gram-positive and Gram-negative bacterial infections and aerobic Staphylococci strains provided that pharmacological activity and risk assessment are carefully performed.


Assuntos
Antibacterianos/farmacologia , Bactérias Anaeróbias/efeitos dos fármacos , Materiais Dentários/farmacologia , Materiais Dentários/toxicidade , Gengiva/efeitos dos fármacos , Nanopartículas Metálicas , Prata/farmacologia , Prata/toxicidade , Antibacterianos/toxicidade , Biofilmes/efeitos dos fármacos , Células Cultivadas , Fibroblastos/efeitos dos fármacos , Gengiva/citologia , Humanos , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Polietilenoglicóis/química , Staphylococcus epidermidis/efeitos dos fármacos , Streptococcus mutans/efeitos dos fármacos , Taninos/química , Ácido Tióctico/química
3.
Acta Pol Pharm ; 73(2): 389-94, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27180431

RESUMO

The study of the sensitivity to tea tree oil (Australian Company TTD International Pty. Ltd. Sydney) was carried out on 193 strains of anaerobic bacteria isolated from patients with various infections within the oral cavity and respiratory tracts. The susceptibility (MIC) of anaerobes was determined by means of plate dilution technique in Brucella agar supplemented with 5% defibrinated sheep blood, menadione and hemin. Inoculum contained 10(5) CFU per spot was cultured with Steers replicator upon the surface of agar with various tea tree oil concentrations or without oil (anaerobes growth control). Incubation the plates was performed in anaerobic jars under anaerobic conditions at 37 degrees C for 48 h. MIC was defined as the lowest concentrations of the essential oil completely inhibiting growth of anaerobic bacteria. Test results indicate, that among Gram-negative bacteria the most sensitive to essential oil were strains of Veillonella and Porphyromonas species. Essential oil in low concentrations (MIC in the range of = 0.12 - 0.5 mg/mL) inhibited growth of accordingly 80% and 68% strains. The least sensitive were strains of the genus Tannerella, Parabacteroides and Dialister (MIC 1.0 - 2.0 mg/mL). In the case of Gram-positive anaerobic bacteria the tea tree oil was the most active to strains of cocci of the genus Anaerococcus and Ruminococcus (MIC in range = 0.12 - 0.5 mg/mL) or strains of rods of the genus Eubacterium and Eggerthella (MIC = 0.25 mg/mL). Among Gram-positive rods the least sensitive were the strains of the genus Bifidobacterium ( MIC = 2.0 mg/mL). The tea tree oil was more active to Gram-positive than to Gram-negative anaerobic bacteria.


Assuntos
Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Óleo de Melaleuca/química , Antibacterianos/isolamento & purificação , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Bactérias Gram-Negativas/classificação , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Negativas/isolamento & purificação , Bactérias Gram-Positivas/classificação , Bactérias Gram-Positivas/crescimento & desenvolvimento , Bactérias Gram-Positivas/isolamento & purificação , Humanos , Fitoterapia , Plantas Medicinais
4.
Pol J Microbiol ; 64(3): 299-305, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26638540

RESUMO

A series of N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidine derivatives bearing sulfonamide moiety have been screened in vitro for antibacterial activity against isolates from patients with infections of oral cavity, respiratory tract and intestinal tract. The majority of compounds exhibited good antibacterial potency. 1-[4-Chloro-5-methyl-2-(4-trifluoromethylbenzylthio)benzenesulfonyl]-3-(3-sulfamoylphenyl)guanidine (13) showed very strong activity, with MIC ≤ 6.2 µg/ml against eleven bacteria strains belonged to Gram-positive anaerobes and aerobes. Furthermore, compound 13 exhibited promising activity toward highly resistant microorganisms such as methicillin-resistant Staphylococcus aureus and Enterococcusfaecalis. It was found that Parvimonas micra, Finegoldia magna, Peptostreptococcus anaerobius, Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Guanidinas/química , Guanidinas/farmacologia , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Infecções Bacterianas/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade
5.
Acta Pol Pharm ; 72(2): 367-75, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26642688

RESUMO

Bronchosol is a traditional medicinal product in the form of syrup used in cough and impeded expectoration. The active ingredients that it contains include extracts from the herb of thyme, the root of primrose and thymol. It is recommended in disorders of the respiratory tract when expectoration is impeded and secretion of liquid mucus in bronchi is insufficient. Antimicrobial activity of the components of Bronchosol, especially thyme and thymol, has frequently been reported in the literature. To date, there have not been any studies to confirm such activity of Bronchosol, though. The results of our research are the first one to point to the great activity of Bronchosol against microorganisms causing infections of the respiratory tract. It has been demonstrated that this product displayed antimicrobial activity against reference strains as well as strains of anaerobic and aerobic bacteria and fungi isolated from patients. The confirmation of the antimicrobial activity of Bronchosol provides an explanation of its effectiveness in the therapy of the respiratory tract infections.


Assuntos
Anti-Infecciosos/farmacologia , Expectorantes/farmacologia , Preparações de Plantas/farmacologia , Primula , Timol/farmacologia , Thymus (Planta) , Testes de Sensibilidade Microbiana
6.
Molecules ; 19(9): 13704-23, 2014 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-25185072

RESUMO

Pathogenic fungi are one of the main causes of hospital-related infections. Since conventional antifungals have become less effective because of the increasing fungal resistance to the standard drugs, the need for new agents is becoming urgent. Herein we report a synthesis of a series of novel N-[imino-(1-oxo-(1H)-phthalazin-2-yl)methyl]-benzenesulfonamide derivatives with in vitro activity against yeast-like fungi isolated from the oral cavity and respiratory tract of patients with candidiasis. These compounds were synthesized by the one-step or two-step reactions of 1-(2-alkylthiobenzensulfonyl)-2-aminoguanidines with the appropriate ortho-carbonyl benzoic acids. The biological study revealed that new derivatives have shown significant growth-inhibitory activity, superior or comparable, than those of the reference drug fluconazole. The most promising activities were observed against Candida albicans, with inhibition at least 1-3 (12.5%-37.5%) of the eight tested strains at the low MIC level of ≤6.2-25 µg/mL.


Assuntos
Antifúngicos/síntese química , Candida albicans/efeitos dos fármacos , Sulfonamidas/síntese química , Antifúngicos/farmacologia , Candida albicans/isolamento & purificação , Candidíase/tratamento farmacológico , Candidíase/microbiologia , Fluconazol/farmacologia , Humanos , Testes de Sensibilidade Microbiana , Boca/microbiologia , Sistema Respiratório/microbiologia , Infecções Respiratórias/tratamento farmacológico , Infecções Respiratórias/microbiologia , Relação Estrutura-Atividade , Sulfonamidas/farmacologia
7.
Acta Pol Pharm ; 71(5): 795-802, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25362808

RESUMO

The antimicrobial activity of sirupus Bioaron C, a preparation, whose main ingredient is an extract from the leaves of Aloe arborescens, was tested against different microorganisms isolated from patients with upper respiratory tract infections. The experiments were performed on 40 strains: 20 strains of anaerobic bacteria, 13 strains of aerobic bacteria and 7 strains of yeast-like fungi from the genus Candida and on 18 reference strains (ATCC). The antimicrobial activity of Bioaron C (MBC and MFC) was determined at undiluted concentration. Bioaron C proved to be very effective against the microorganisms causing infections. At the concentration recommended by the producer, the preparation showed biocidal activity (MBC, MFC) against the strains of the pathogenic microorganisms, which cause respiratory infections most frequently, including, among others, Peptostreptococcus anaerobius, Parvimonas micra, Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus anginosus, Haemophilus influenzae, Moraxella catarrhalis, Pseudomonas aeruginosa and Candida albicans, already after 15 min. The MIC of Bioaron C against most of the tested microorganisms was 5 to 100 times lower than the usually applied concentration. The great antimicrobial activity means that the preparation may be used in the prevention and treatment of infections of the upper respiratory tract. Bioaron C may be an alternative or complement to classical therapy, especially in children.


Assuntos
Aloe/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Extratos Vegetais/farmacologia , Infecções Respiratórias/tratamento farmacológico , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Humanos , Pneumopatias Fúngicas/tratamento farmacológico , Pneumopatias Fúngicas/microbiologia , Testes de Sensibilidade Microbiana , Fitoterapia , Plantas Medicinais , Infecções Respiratórias/microbiologia
8.
J Enzyme Inhib Med Chem ; 28(1): 41-51, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22145585

RESUMO

Few series of novel 4-chloro-2-mercaptobenzenesulfonamides have been synthesized by the reactions of N-(benzenesulfonyl)cyanamide potassium salts 7-15 with corresponding hydrazinecarbodithioic acid esters, 1-substituted carbothioic acid hydrazides, methyl 3-aminothiophene-2-carboxylate, methyl 2-aminobenzoate, 2-aminophenol or 2-aminothiophenol. The synthesized compounds (16-49) were screened in vitro for their antibacterial activity. Some of the tested compounds 16, 17, 23, 24, 31, 32 and 48 showed the promising activity against many of anaerobic Gram-positive bacteria strains.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Sulfonamidas/química , Aminofenóis/química , Compostos de Anilina/química , Antibacterianos/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Técnicas de Química Sintética , Ciclização , Ensaios de Seleção de Medicamentos Antitumorais , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade
9.
Przegl Lek ; 66(7): 373-9, 2009.
Artigo em Polonês | MEDLINE | ID: mdl-20043579

RESUMO

INTRODUCTION: In the last years literature has paid attention to positive correlation between periodontitis and coronary heart disease, acute coronary events, including myocardial infarction. Mechanisms of this relationship are not completely known. One of the research trends for elucidation of these problems are bacteriological studies. The aim of this study was qualitative and quantitative evaluation of bacterial flora of the periodontal pocket in patients with coronary heart disease and myocardial infarction, with co-existing periodontitis. MATERIAL AND METHODS: The research included 40 patients, hospitalised in 1st Clinic of Cardiology, Medical University in Gdansk. Group 1 included 20 patients after myocardial infarction, group 2 of 20 patients with diagnosed coronary heart disease, with many years duration without acute events. Control group encompassed 20 patients of Chair and Department of Periodontology and Oral Mucosa Diseases, Medical University in Gdansk, without cardiovascular diseases. Inclusion criterion for the study was diagnosed chronic periodontitis in all patients. In clinical evaluation indices: API, SBI, PD and CAL were used. The material for bacteriological research was taken in each patient from 4 periodontal pockets, minimum 5 mm depth. The culture and identification were performed with present principles. Based on the litearture data about potential pathogenicity for periodontium and cardiovascular system, species for analyse were chosen. RESULTS: Statistical analyse proved equality of evaluated groups and control group in gender, age and estimated clinical indices. In periodontal pockets all patients anaerobic flora dominated, however without significiant differences in species range. Among microaerophilia and streptococci statistical analyse showed significiant differences in frequency of isolation of Actinobacillus actinomycetescomitans and Streptococcus sanguis in group 1 in comparision to group 2 and control group. Quantitative analyse showed no significiant differences between groups for all bacteria species. CONCLUSIONS: Clinical evaluation showed comparable values of periodontal parameters. The bacteria species Porphyromonas gingivalis, Actinobacillus actinomycetescomitans and Streptococcus sanguis were more often isolated from periodontal pockets in persons after myocardial infarction, statistically significant for A.a. and S.s.


Assuntos
Bolsa Periodontal/microbiologia , Aggregatibacter actinomycetemcomitans/isolamento & purificação , Doença Crônica , Doença das Coronárias/complicações , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Infarto do Miocárdio/complicações , Streptococcus sanguis/isolamento & purificação
10.
Pol J Microbiol ; 55(4): 303-7, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-17416067

RESUMO

Yeast-like fungi are the most common cause of fungal infections in humans. Actually, in the age of opportunistic infections and increasing resistance, development of modern antifungal agents becomes a very important challenge. This paper describes synthesis and antimicrobial assay of four naturally occurring peptide antibiotics (aurein 1.2, citropin 1.1, temporin A, uperin 3.6) and three chemically engineered analogues actually passing clinical trials (iseganan, pexiganan, omiganan) against Candida strains isolated from patients with infections of the oral cavity or respiratory tract. The peptides were synthesized using solid-phase method and purified by high-performance liquid chromatography. Biological tests were performed using the broth microdilution method. The antifungal activity of the peptide antibiotics was compared to that of nystatin and amphotericin B. We found synthetic peptides to be generally less potent than amphotericin B or nystatin. However, some of the naturally occurring peptides still retained reasonable antifungal activities which were higher than these of iseganan, pexiganan or omiganan. We think that the naturally occurring peptide antibiotics included in our study can be a good matrix for development of novel antifungal compounds.


Assuntos
Antifúngicos/farmacologia , Peptídeos Catiônicos Antimicrobianos/farmacologia , Candida/efeitos dos fármacos , Candida/isolamento & purificação , Candidíase Bucal/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Infecções Respiratórias/microbiologia
11.
Acta Pol Pharm ; 63(1): 39-45, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-17515328

RESUMO

The new pyrazine derivatives exhibiting an antibacterial activity have been synthesized. Initial amidoxime 1 was obtained in the reaction of pyrazinecarbonitrile with hydroxylamine. Upon treatment of amidoxime with methyl iodide O-methyl derivative 2 was formed. Both amidoximes were transformed into imidoyl chlorides 3, 4. Then the chloride atom in those derivatives was substituted with various secondary amines giving appropriate oximes 5-18 and O-methyl-oximes 19 and 20. The obtained compounds were tested in vitro for their tuberculostatic activity. The inhibiting concentration (MIC) values were within 25-100 microg/mL. Their activity towards 25 strains of anaerobic and 25 strains of aerobic bacteria was also studied. Three compounds exhibited activity against both types of bacteria.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Oximas/síntese química , Oximas/farmacologia , Pirazinas/síntese química , Pirazinas/farmacologia , Bactérias/efeitos dos fármacos , Bactérias Aeróbias/efeitos dos fármacos , Bactérias Anaeróbias/efeitos dos fármacos , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Espectrofotometria Infravermelho , Relação Estrutura-Atividade
12.
Przegl Lek ; 63(5): 257-60, 2006.
Artigo em Polonês | MEDLINE | ID: mdl-17036500

RESUMO

UNLABELLED: Frequency of occurrence of mycotic infections of the oral mucosa is higher in later years. It is connected with common use of antibiotics, intensive cancer treatment (cytostatics, radiation therapy) as well as immunosuppressant drugs and antibiotics, which have an influence on mikroflora disorders of the oral cavity. Candidiasis of oral mucosa occurs in old patients, in people suffering from diabetes mellitus, hypothyreosis, sideropenia, hypovitaminosis and xerostomia, which is often caused by hypofunction of salivary glands during autoimmune diseases and/or drug and systemic treatment. The aim of the study was to make a retrospective evaluation of frequency of occurring mycotic infections in patients treated in the Department of Periodontology and Oral Mucosa Diseases, Medical University of Gdansk in the 2003, as well as recognition of systemic conditioning of these disorders. The Study material was clinical documentation of 4172 patients, treated because of different oral mucose and periodontium disorders. From these patients, selected was a group of 105 (83 women and 22 men) with diagnosis--Candidosis mucosae oris. Clinical and mycotic examination was performed. RESULTS: Mycotic infections were found in 105 patients (2.5%). Systemic diseases (74.3%) were found in a maturity of the patients, which indicated systemic predispositions to candida infections. CONCLUSION: A wide cooperation between general practitioners and dentists, especially perio-dontologists, is necessary to give full care to patients. Early diagnosis of disorders of the oral cavity of patients with systemic diseases and dentistry treatment or taking preventive measures seems to be necessary.


Assuntos
Candidíase Bucal/epidemiologia , Candidíase Bucal/etiologia , Adolescente , Adulto , Distribuição por Idade , Idoso , Idoso de 80 Anos ou mais , Antibacterianos/efeitos adversos , Antineoplásicos/efeitos adversos , Asma/epidemiologia , Doenças Cardiovasculares/epidemiologia , Causalidade , Comorbidade , Doenças do Sistema Endócrino/epidemiologia , Doenças do Sistema Endócrino/terapia , Feminino , Humanos , Comunicação Interdisciplinar , Masculino , Pessoa de Meia-Idade , Neoplasias/epidemiologia , Neoplasias/terapia , Radioterapia/efeitos adversos , Estudos Retrospectivos , Doenças Reumáticas/epidemiologia , Distribuição por Sexo
13.
Int J Angiol ; 25(1): 3-13, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-26900306

RESUMO

There are an increasing number of data showing a clinically important association between bacterial infection and peripheral artery disease (PAD). Bacteria suspected of being involved in PAD pathogenesis are: periodontal bacteria, gut microbiota, Helicobacter pylori, and Chlamydia pneumoniae. Infectious agents may be involved in the pathogenesis of atherosclerosis via activation of a systemic or local host immunological response to contamination of extravascular tissues or the vascular wall, respectively. A systemic immunological reaction may damage vascular walls in the course of autoimmunological cross-reactions between anti-pathogen antibodies and host vascular antigens (immunological mimicry), pathogen burden mechanisms (nonspecific activation of inflammatory processes in the vascular wall), and neuroendocrine-immune cross-talk. Besides activating the inflammatory pathway, bacterial infection may trigger PAD progression or exacerbation by enhancement of platelet reactivity, by a stimulatory effect on von Willebrand factor binding, factor VIII, fibrinogen, P-selectin activation, disturbances in plasma lipids, increase in oxidative stress, and resistance to insulin. Local inflammatory host reaction and induction of atherosclerotic plaque progression and/or instability result mainly from atherosclerotic plaque colonization by microorganisms. Despite these premises, the role of bacterial infection in PAD pathogenesis should still be recognized as controversial, and randomized, controlled trials are required to evaluate the outcome of periodontal or gut bacteria modification (through diet, prebiotics, and probiotics) or eradication (using antibiotics) in hard and surrogate cardiovascular endpoints.

14.
Med Chem ; 12(7): 640-646, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27184263

RESUMO

BACKGROUND: Cutaneous and invasive fungal infections are constant threats to human health that substantiate the need for the development of new efficacious and safe antimycotics. METHODS: A series of N1-alkyl, N1-acyl and N1-sulfonyl derivatives of 4,6- dimethylisoxazolo[3,4-b]pyridin-3(1H)-one (1) were synthesized. The antimicrobial activities of title compounds against 21 pathogenic yeast-like fungal clinical isolates and 5 reference strains were evaluated by means of a broth microdilution method. RESULTS: Among the compounds tested, the newly prepared N1-benzoyl (2m) and N1-(4-fluorobenzoyl) (2n) derivatives of 1 showed 81% and 95% inhibitory efficacy, respectively, against the clinical isolates, which were comparable to that of the reference drug fluconazole. The strains that exhibited the highest susceptibility to the compound 2n included Candida utilis (MIC < 6.2 µg/mL), C. parapsilosis (MIC in the range <6.2 - 12.5 µg/mL), Geotrichum candidum (MIC = 12.5 µg/mL) as well as C. lusitaniae and Rhodotorula mucilaginosa (MIC = 25 µg/mL). CONCLUSION: In terms of MIC, compound 2n proved to be four times more active against the clinical isolates of Candida albicans and C. albicans ATCC 10231 standard strain than fluconazole, the widely prescribed antifungal agent for mucosal and systemic yeast infections (MIC = 50 vs 200 µg/mL).


Assuntos
Antifúngicos/farmacologia , Isoxazóis/farmacologia , Piridonas/farmacologia , Antifúngicos/síntese química , Candida/efeitos dos fármacos , Geotrichum/efeitos dos fármacos , Isoxazóis/síntese química , Testes de Sensibilidade Microbiana , Piridonas/síntese química , Rhodotorula/efeitos dos fármacos , Saccharomyces cerevisiae/efeitos dos fármacos
15.
Farmaco ; 60(6-7): 513-7, 2005.
Artigo em Inglês | MEDLINE | ID: mdl-15950227

RESUMO

The investigations of new pyrazine and pyridine derivatives showing an antibacterial activity have been made. Upon treatment of 3-chloro-2-cyanopyrazine [1] and 2-chloro-3-cyanopyridine with 1,1-dimethyl-hydrazine, 1-aminopiperidine and 1-amino-4-methylpiperazine, either the pyrazolo-pyrazine (1), and -pyridine (2) derivatives, or ammonium salts (3-8) were obtained, according to the reaction conditions. Compound 1 was obtained in the reaction of the initial nitrile with methylhydrazine as well. The reactions of 1 gave the following derivatives: acylation-(9), that with p-chlorobenzoic aldehyde-(10), and with phenyl-isothiocyanate-(11). 3-Chloro-2-cyanopyrazine treated with hydrazine hydrate gave amidrazone (12), which upon condensation with p-chlorobenzoic aldehyde produced (13). The compounds obtained were tested in vitro for their tuberculostatic activity. The minimal inhibitory concentration (MIC) values were within 22-100 microg/cm3. Compounds 1, 5 and 6 were also tested in vitro for their activity towards 25 strains of anaerobic, and 25 strains of aerobic bacteria. They appeared to be of elevated activity towards the anaerobes and of low one towards the aerobes (Table 2).


Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Pirazóis/farmacologia , Piridinas/farmacologia , Antibacterianos/síntese química , Bactérias Anaeróbias Gram-Negativas/efeitos dos fármacos , Metronidazol/farmacologia , Testes de Sensibilidade Microbiana/métodos , Modelos Químicos , Pirazóis/síntese química , Piridinas/síntese química
16.
Med Dosw Mikrobiol ; 57(2): 209-15, 2005.
Artigo em Polonês | MEDLINE | ID: mdl-16134393

RESUMO

The aim of this study was to assess the occurrence of microorganisms in 39 intraoral abscesses. The samples were place in transport medium. The materials were inoculated on adequate enrichment and selective media and cultivated under anaerobic and aerobic conditions. The microorganisms were found in all samples (100%), Anaerobic bacteria most frequently were recovered. The predominant anaerobes were from genus Prevotella, Bacteroides, Fusobacterium and Peptostreptococcus. Among aerobic bacteria, the most frequent were gram-positive cocci. The microaerophilic bacteria and fungi most rarely were isolated from pus samples.


Assuntos
Abscesso/microbiologia , Bactérias Aeróbias/isolamento & purificação , Bactérias Anaeróbias/isolamento & purificação , Estomatite/microbiologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Bacteroides/isolamento & purificação , Feminino , Fusobacterium/isolamento & purificação , Humanos , Masculino , Pessoa de Meia-Idade , Peptostreptococcus/isolamento & purificação , Prevotella/isolamento & purificação
17.
Med Dosw Mikrobiol ; 55(2): 173-80, 2003.
Artigo em Polonês | MEDLINE | ID: mdl-14577197

RESUMO

Purpose of this study was to find out what kind of anaerobic bacteria were in lower respiratory tract and how often they were present there considering patients after thoracic surgery. Also, what is susceptibility of bacteria to antibiotics. Research covered 30 patients after operation. Material for research was bronchoalveolar lavage (BAL) taken during bronchoscopy. Collected sample was cultivated in anaerobic and aerobic conditions. Anaerobic bacteria were found in 28 samples (93%). Totally there were 100 anaerobic bacteria strains. The most common Gram-negative rods were from genus Prevotella (24 strains, 24%) and Bacteroides (15 strains, 15%). Gram-negative bacteria except Bacteroides characterised biggest susceptibility to imipenem, piperacillin/tazobactam, amoxicillin/clavulanate, ampicillin/sulbactam, piperacillin, clindamycin and metronidazol. Bacteroides were susceptible to imipenem, piperacillin/tazobactam and metronidazol. Among Gram-positive anaerobic bacteria mostly were isolated from cocci Peptostreptococcus (18 strains, 18%) and were susceptible to all antibiotics. Gram-positive rods were in most cases represented by Actinomyces (12 strains 12%) and were highly susceptible to all antibacterial means except metronidazol (100% is resistant).


Assuntos
Bactérias Anaeróbias/isolamento & purificação , Líquido da Lavagem Broncoalveolar/microbiologia , Procedimentos Cirúrgicos Torácicos , Idoso , Animais , Anti-Infecciosos/farmacologia , Bactérias Anaeróbias/efeitos dos fármacos , Farmacorresistência Bacteriana , Feminino , Bactérias Anaeróbias Gram-Negativas/isolamento & purificação , Bactérias Gram-Positivas/isolamento & purificação , Humanos , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade
18.
Pneumonol Alergol Pol ; 71(1-2): 68-73, 2003.
Artigo em Polonês | MEDLINE | ID: mdl-12959026

RESUMO

Anaerobic bacteria are predominant components of normal oral cavity, upper respiratory tract, gastrointestinal, genital and skin flora. They are involved in infections such as pneumonia, aspiration pneumonia, lung abscess and empyema. Laboratory diagnosis of anaerobic infections is based on recovering the etiological agents from clinical materials. Appropriatte specimens include: pus, purulent fluid, biopsy specimen of lung, transtracheal aspirates and bronchoalveolar lavage (BAL). Lower respiratory infections are usually either polymicrobial or mixed anaerobic-aerobic infections. Peptostreptococcus, Fusobacterium, Prevotella and Bacteroides are the most common anaerobes. Anaerobic bacteria are susceptible to metronidazole, tinidazole (exception of Gram-positive rods), amoxicillin/clavulanate, ampicillin/sulbactam, piperacillin/tazobactam, imipenem and clindamycin. Treatment includes an antibiotics regimen with an agent active against anaerobic and aerobic bacteria (therapy with 2 or 3 antimicrobial drugs).


Assuntos
Bactérias Anaeróbias/isolamento & purificação , Líquidos Corporais/microbiologia , Infecções Respiratórias/microbiologia , Antibiose , Bactérias Anaeróbias/efeitos dos fármacos , Bacteroides/efeitos dos fármacos , Bacteroides/isolamento & purificação , Exsudatos e Transudatos/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Prevotella/efeitos dos fármacos , Prevotella/isolamento & purificação
19.
Pneumonol Alergol Pol ; 71(1-2): 51-8, 2003.
Artigo em Polonês | MEDLINE | ID: mdl-12959024

RESUMO

Purpose of this study was to analyse the kind and frequency of anaerobic bacteria in the lower respiratory tract as well as susceptibility of the bacteria to antibiotics. Material from 35 patients with lung tumour derived from tumour and post-tumoural area sample. Collected sample was cultivated in anaerobic and aerobic conditions. Anaerobic bacteria were found in 23 (66%) samples. Totally there were 44 isolated of anaerobic bacteria strains. The most common G-negative strains belonged to genus of Bacteroides (11 strains); two types dominated: Bacteroides gracilis (4 strains) Bacteroides fragilis (4 strains). Among G-positive anaerobic bacteria most common were Peptostreptococcus (9 strains). G-positive rods were represented by Propionibacterium genus (8 strains). The susceptibility of anaerobic bacteria was estimated towards mostly used antibacterial drugs. Results suggest that most of bacteria were susceptible for imipenem, piperacillin/tazobactam, amoxicillin/clavulanate, ampicillin/sulbactam, metronidazole, piperacillin and clindamycin. Bacteria were less susceptible to roxitromycin and examined cephalosporins. Most of the strains were resistant for cefuroxime.


Assuntos
Bactérias Anaeróbias/classificação , Bactérias Anaeróbias/isolamento & purificação , Neoplasias Pulmonares/microbiologia , Adulto , Idoso , Resistência a Medicamentos , Feminino , Humanos , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade
20.
Przegl Lek ; 61(5): 467-72, 2004.
Artigo em Polonês | MEDLINE | ID: mdl-15515807

RESUMO

Cyclosporine A (CsA) is one of the basic and often used immunosuppressive agents. It is used to prevent rejection of allogenic transplants and to cure many diseases with autoimmunological components. The development of transplantology and frequent presence of autoaggressive disorders causes increased use of CsA, which intensifies problem of side-effects. Gingival overgrowth, oral mucosa pathologies related with bacterial, viral and fungal infections and neoplasma are described as most frequent side-effects of cyclosporine A in the oral cavity. The aim of this study was to assess the frequency of presence of different types of oral mucosa lesions in cyclosporine A-treated patients after renal transplantation. Thirty renal transplant recipients aged 11-64 years (including 13 females and 17 males) with cyclosporine treatment period from 6 months to 10 years were examined. Pathological changes on the oral mucosa were noted in 18 patients (60%). The fungal infections were the most often observed pathology (46.7% of examined persons). In mycological tests Candida albicans was most often isolated. Other species: C. kefyr, C. parapsilosis and C. tropicalis were also found. In 4 cases cheilitis angularis was additionally diagnosed. In 16.7% of CsA-treated patients, pathological changes of epithelium with homogenic leucoplakia features were observed. Hypertrophic lesions of oral mucosa in 10% of cases and many small erosions of inflamed mucosa of hard palate in 1 case were also noted. Our observations show connection between incidence of oral mucosa pathologies and immunosuppressive treatment. This suggests that interdisciplinary cooperation is necessary for early start of prevention and treatment program.


Assuntos
Ciclosporina/efeitos adversos , Transplante de Rim , Mucosa Bucal , Adolescente , Adulto , Candidíase/etiologia , Queilite/etiologia , Criança , Feminino , Crescimento Excessivo da Gengiva/etiologia , Humanos , Imunossupressores/efeitos adversos , Falência Renal Crônica/cirurgia , Leucoplasia/etiologia , Masculino , Pessoa de Meia-Idade , Mucosa Bucal/efeitos dos fármacos , Mucosa Bucal/microbiologia , Mucosa Bucal/patologia , Mucosa Bucal/virologia
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