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1.
Saudi J Biol Sci ; 31(4): 103965, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38440744

RESUMO

Cosmetic products may be exposed to microbial contamination during storage or transport, and to avoid the risk of microbial growth, manufacturers add preservative compounds as a protection for the product from spoilage. The Microbial Challenge test is a procedure to evaluate the preservative efficacy by challenging the product with testing microorganisms to determine the quality of preservation. In this study, thirty-two cosmetics products used for body and skin care were collected from markets and pharmacies in Mecca region, these products are subjected to microbiological analysis, results show that most samples are contaminated except six samples. Non contaminated samples were subjected to European Pharmacopeia 7.0 standards. Results show that two samples, foaming gel and body and face cream are failed to demonstrate the required microbiocidal effect against the S.aureus test species, results recorded 1.21 x 105 and 6.80 x 105 (CFU/ml) respectively at the second day of incubation, other products: shower gel, hand wash, body lotion and shampoo demonstrate that required microbiocidal effect against the test species during day 2, 7, 14 until day 28th. The microbial count number is less than 10 during all incubation periods. To prevent contamination in cosmetics, manufacturers are required to add a good preservative system to the products and examine them before sale. Due to the high percentage of microbial contamination in cosmetics in Mecca region and for consumers safety, this study is prepared.

2.
AMB Express ; 14(1): 27, 2024 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-38381255

RESUMO

The operative mechanisms and advantageous synergies existing between the rhizobiome and the wild plant species Abutilon fruticosum were studied. Within the purview of this scientific study, the reservoir of genes in the rhizobiome, encoding the most highly enriched enzymes, was dominantly constituted by members of phylum Thaumarchaeota within the archaeal kingdom, phylum Proteobacteria within the bacterial kingdom, and the phylum Streptophyta within the eukaryotic kingdom. The ensemble of enzymes encoded through plant exudation exhibited affiliations with 15 crosstalking KEGG (Kyoto Encyclopaedia of Genes and Genomes) pathways. The ultimate goal underlying root exudation, as surmised from the present investigation, was the biosynthesis of saccharides, amino acids, and nucleic acids, which are imperative for the sustenance, propagation, or reproduction of microbial consortia. The symbiotic companionship existing between the wild plant and its associated rhizobiome amplifies the resilience of the microbial community against adverse abiotic stresses, achieved through the orchestration of ABA (abscisic acid) signaling and its cascading downstream effects. Emergent from the process of exudation are pivotal bioactive compounds including ATP, D-ribose, pyruvate, glucose, glutamine, and thiamine diphosphate. In conclusion, we hypothesize that future efforts to enhance the growth and productivity of commercially important crop plants under both favorable and unfavorable environmental conditions may focus on manipulating plant rhizobiomes.

3.
Biomolecules ; 13(12)2023 11 21.
Artigo em Inglês | MEDLINE | ID: mdl-38136554

RESUMO

COVID-19, caused by the SARS-CoV-2 virus, manifests with a wide range of clinical symptoms that vary from mild respiratory issues to severe respiratory distress. To effectively manage and predict the outcomes of the disease, it is important to understand the molecular mechanisms underlying its severity. This study focuses on analyzing and comparing the expression patterns of microRNAs (miRNAs) in serum, urine, and nasopharyngeal samples from patients with mild, moderate, and severe COVID-19. The aim is to identify potential associations with disease progression and discover suitable markers for diagnosis and prognosis. Our findings indicate the consistent upregulation of miR-21, miR-146a, and miR-155 in urine, serum, and nasopharyngeal samples from patients with mild COVID-19. In moderate cases, there were more significant changes in miRNA expression compared to mild cases. Specifically, miR-let-7 demonstrated upregulation, while miR-146b exhibited downregulation. The most notable alterations in miRNA expression profiles were observed in severe COVID-19 cases, with a significant upregulation of miR-223. Moreover, our analysis using Receiver-operating characteristic (ROC) curves demonstrated that miR-155, miR-let-7, and miR-223 exhibited high sensitivity and specificity, suggesting their potential as biomarkers for distinguishing COVID-19 patients from healthy individuals. Overall, this comparative analysis revealed distinct patterns in miRNA expression. The overlapping expression patterns of miRNAs in urine, serum, and nasopharyngeal samples suggest their potential utility in discriminating disease status.


Assuntos
COVID-19 , MicroRNAs , Humanos , COVID-19/diagnóstico , COVID-19/genética , SARS-CoV-2/genética , SARS-CoV-2/metabolismo , MicroRNAs/metabolismo , Biomarcadores , Curva ROC
4.
Saudi J Biol Sci ; 30(12): 103852, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38020232

RESUMO

Cosmetic products contain several components that are ideal for microbial growth, they exposed to contamination by pathogenic bacteria and fungi, and this may cause health risks such as skin and eye infections. In this investigation, 50 samples were obtained from various shops in Mecca region, Saudi Arabia. Collected samples include high-quality and low-quality brands of makeup. Results show that most cosmetics are contaminated with microorganisms. Bacterial and fungal isolates were identified by morphological and microscopic techniques, and confirmed by molecular methods: (16s rRNA) for bacterial isolates and (18s rRNA) for fungal isolates associated with cosmetics. In low-quality cosmetics, frequency of microbial growth is higher and more diverse than high-quality cosmetics. It has been observed the most contaminated product was in lip gloss and it follows by the lipstick. The most predominant species of bacteria are Staphylococcus aureus (27 %), E. coli (27 %), which follows by Streptococcus pneumonia (18 %), Staphylococcus epidermis (17 %), Bacilli subtilis (12 %), and Pseudomonas aeruginosa (5 %). Aspergillus sp is the most predominant fungi (57 %), which is followed by Penicillium sp. (29 %) and Rhizopus sp. (14 %). In high quality brands, the frequency of microbial growth was the highest in mascara, lip-gloss. The most predominant species of bacteria is Staphylococcus aureus (41 %), which follows by Bacilli subtilis and Pseudomonas aeruginosa and E. coli (17 %). Streptococcus pneumonia is the less dominant (5 %). There is no growth on media of fungi. Due to the large number of cosmetics brands in Mecca region and for consumer safety, this study is prepared.

6.
AMB Express ; 13(1): 92, 2023 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-37646836

RESUMO

A metagenomic whole genome shotgun sequencing approach was used for rhizospheric soil micribiome of the wild plant Abutilon fruticosum in order to detect antibiotic resistance genes (ARGs) along with their antibiotic resistance mechanisms and to detect potential risk of these ARGs to human health upon transfer to clinical isolates. The study emphasized the potential risk to human health of such human pathogenic or commensal bacteria, being transferred via food chain or horizontally transferred to human clinical isolates. The top highly abundant rhizospheric soil non-redundant ARGs that are prevalent in bacterial human pathogens or colonizers (commensal) included mtrA, soxR, vanRO, golS, rbpA, kdpE, rpoB2, arr-1, efrA and ileS genes. Human pathogenic/colonizer bacteria existing in this soil rhizosphere included members of genera Mycobacterium, Vibrio, Klebsiella, Stenotrophomonas, Pseudomonas, Nocardia, Salmonella, Escherichia, Citrobacter, Serratia, Shigella, Cronobacter and Bifidobacterium. These bacteria belong to phyla Actinobacteria and Proteobacteria. The most highly abundant resistance mechanisms included antibiotic efflux pump, antibiotic target alteration, antibiotic target protection and antibiotic inactivation. antimicrobial resistance (AMR) families of the resistance mechanism of antibiotic efflux pump included resistance-nodulation-cell division (RND) antibiotic efflux pump (for mtrA, soxR and golS genes), major facilitator superfamily (MFS) antibiotic efflux pump (for soxR gene), the two-component regulatory kdpDE system (for kdpE gene) and ATP-binding cassette (ABC) antibiotic efflux pump (for efrA gene). AMR families of the resistance mechanism of antibiotic target alteration included glycopeptide resistance gene cluster (for vanRO gene), rifamycin-resistant beta-subunit of RNA polymerase (for rpoB2 gene) and antibiotic-resistant isoleucyl-tRNA synthetase (for ileS gene). AMR families of the resistance mechanism of antibiotic target protection included bacterial RNA polymerase-binding protein (for RbpA gene), while those of the resistance mechanism of antibiotic inactivation included rifampin ADP-ribosyltransferase (for arr-1 gene). Better agricultural and food transport practices are required especially for edible plant parts or those used in folkloric medicine.

7.
Front Microbiol ; 14: 1166148, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37260683

RESUMO

Introduction: The study aims to describe phageome of soil rhizosphere of M.oleifera in terms of the genes encoding CAZymes and other KEGG enzymes. Methods: Genes of the rhizospheric virome of the wild plant species Moringa oleifera were investigated for their ability to encode useful CAZymes and other KEGG (Kyoto Encyclopedia of Genes and Genomes) enzymes and to resist antibiotic resistance genes (ARGs) in the soil. Results: Abundance of these genes was higher in the rhizospheric microbiome than in the bulk soil. Detected viral families include the plant viral family Potyviridae as well as the tailed bacteriophages of class Caudoviricetes that are mainly associated with bacterial genera Pseudomonas, Streptomyces and Mycobacterium. Viral CAZymes in this soil mainly belong to glycoside hydrolase (GH) families GH43 and GH23. Some of these CAZymes participate in a KEGG pathway with actions included debranching and degradation of hemicellulose. Other actions include biosynthesizing biopolymer of the bacterial cell wall and the layered cell wall structure of peptidoglycan. Other CAZymes promote plant physiological activities such as cell-cell recognition, embryogenesis and programmed cell death (PCD). Enzymes of other pathways help reduce the level of soil H2O2 and participate in the biosynthesis of glycine, malate, isoprenoids, as well as isoprene that protects plant from heat stress. Other enzymes act in promoting both the permeability of bacterial peroxisome membrane and carbon fixation in plants. Some enzymes participate in a balanced supply of dNTPs, successful DNA replication and mismatch repair during bacterial cell division. They also catalyze the release of signal peptides from bacterial membrane prolipoproteins. Phages with the most highly abundant antibiotic resistance genes (ARGs) transduce species of bacterial genera Pseudomonas, Streptomyces, and Mycobacterium. Abundant mechanisms of antibiotic resistance in the rhizosphere include "antibiotic efflux pump" for ARGs soxR, OleC, and MuxB, "antibiotic target alteration" for parY mutant, and "antibiotic inactivation" for arr-1. Discussion: These ARGs can act synergistically to inhibit several antibiotics including tetracycline, penam, cephalosporin, rifamycins, aminocoumarin, and oleandomycin. The study highlighted the issue of horizontal transfer of ARGs to clinical isolates and human gut microbiome.

8.
Saudi J Biol Sci ; 30(2): 103559, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36718281

RESUMO

Staphylococcal protein A (SPA) is an important virulence factor that enables Staphylococcus aureus to evade host immune responses. The current work aims to detect the S. aureus SPA gene by a colorimetric method based on gold nanoparticles (AuNPs). For this purpose, the chromosomal DNA of S. aureus was extracted. Thereafter, primers and thiolated oligonucleotide probe were designed based on protein A sequence data in the gene bank. PCR analysis was performed, and the PCR product was electrophoresed on 2 % agarose gel. Gold nanosensor (Au-Ns) was synthesized by the reaction between AuNPs and the thiolated oligonucleotide probe. The physicochemical properties of AuNPs and Au-Ns were characterized. The detection of the SPA gene was performed based on color change detected by the naked eye and UV-vis spectrophotometry. Finally, the described method was optimized and validated for standard, clinical, and food samples. The PCR analysis showed a characteristic fragment of the SPA gene with a molecular size of 545 base pairs (bp) and a detection limit of 60 pg/ µL. The physicochemical analyses illustrated Au-Ns' correct preparation with a zeta potential of -13.42 mV and particle size range 6-11 nm. Moreover, Au-Ns showed 100 % specificity with a detection limit (DL) of 6 fg/ µL. The proposed method was well described to be applied in clinical and research laboratories.

9.
Pak J Biol Sci ; 25(6): 531-536, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36098188

RESUMO

<b>Background and Objectives:</b> Bacterial cellulose (BC) is a microbial extracellular biopolymer formed by microbial strains like <i>Gluconacetobacter xylinus</i>. The objective of this study was to determine the antioxidant and anticoagulant of a microbial nano cellulose-ZnO-Ag (CNCs) composite and its components separately. <b>Materials and Methods:</b> Three components were used for nano cellulose-ZnO-Ag composite synthesis, Ag-nanoparticles, ZnO-nanoparticles and BC. The DPPH method was used to calculate the scavenging of free radical behaviour of four different composite samples. <b>Results:</b> Results of silver nanoparticles were found to have the highest antioxidant activity with IC<sub>50</sub> 65 µg mL<sup></sup><sup>1</sup>, followed by CNCs-ZnO-Ag composite (IC<sub>50</sub> 88.98 µg mL<sup></sup><sup>1</sup>) but ZnONPs IC<sub>50</sub> was 263 µg mL<sup></sup><sup>1</sup> and BC (IC<sub>50</sub> 955 µg mL<sup></sup><sup>1</sup>). The CNCs-ZnO-Ag composite, BC and AgNPs at 25 µg mL<sup></sup><sup>1</sup> had clotting times that were nearly identical to the control. The APTT increased to 56 Sec at 75 µg mL<sup></sup><sup>1</sup> of CNCs-ZnO-Ag composite related to control that recorded 33 Sec. <b>Conclusion:</b> Bacterial cellulose acquired new activity in nano form and also when conjugated with nanoparticles. The CNCs-ZnO-Ag composite is ready for pharmaceutical application as an antioxidant and anticoagulant after <i>in vivo</i> study.


Assuntos
Nanopartículas Metálicas , Óxido de Zinco , Anticoagulantes/farmacologia , Antioxidantes/farmacologia , Bactérias , Celulose , Prata
10.
Clin Epidemiol Glob Health ; 13: 100935, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34934849

RESUMO

INTRODUCTION: Public awareness regarding COVID-19 plays an important role in controlling the virus' spread and treating infected people. A high level of awareness among the public will help to implement preventive measures, particularly in the most populated regions, such as Makkah, Saudi Arabia. COVID-19 is an infectious disease and the Saudi Arabian government has taken serious precautions and implemented several preventive measures. In addition, The Ministry of Health (MOH) has launched many awareness campaigns and provided COVID-19 vaccines for free. THE OBJECTIVES: To assess the Public's level of health awareness and knowledge toward SARS-CoV-2 and COVID-19 vaccines among residents of Makkah, Saudi Arabia. METHODS: A cross-sectional study was conducted in the Makkah region from February 23 to March 2, 2021. The questionnaire was generated using a Google form and distributed online through social platforms such as Twitter and WhatsApp. The questionnaire consisted of five sections and six hundred participants have answered and completed all questions. Then, All data were imported into Microsoft Excel and analyzed using the statistical tools SAS version 9.4 and SPSS version 25 software. RESULTS: A total of 600 participants from the Makkah region were found to have a high level of awareness and knowledge about all aspects of SARS-CoV-2 and the COVID-19 disease. For example, all participants considered coronavirus to be contagious, and 89.8% of them knew that COVID-19's symptoms are similar to those of seasonal flu. Most respondents showed a high level of awareness regarding the main factors of SARS-CoV-2 transmission. Over 98.7% of respondents were aware of the role of gatherings and events in further spread of the virus. The participants showed a good level of awareness about other preventive measures, such as maintaining social distancing and wearing a mask. However, the respondents considered COVID-19 vaccines to be effective, but some of them were not aware of their side effects, and 38.8% planned to receive a vaccine. CONCLUSION: The residents of Makkah showed a high level of awareness about these aspects; an excellent awareness level was noted for SARS-CoV-2, means of transmission, disease symptoms and prevention of viral spread. On the other hand, the participants had less knowledge regarding COVID-19 vaccines; hence, more effort is required to educate people about the safety and benefits of the vaccines.

11.
Ecotoxicol Environ Saf ; 222: 112521, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34274835

RESUMO

An Egyptian rhizobacterium Azospirillum sp. isolated from Sadat city was able to produce indole acetic acid (IAA) up to (30.59 µg/ml). The isolate was identified biochemically and by 16S rRNA sequencing which showed 99.9% similarity to Azospirillum brasilense. The new isolate has been registered in Genbank with accession number MH179119.1. Extracted IAA was used as reducing or stabilizing agent of sliver nanoparticles (AgNPs). Successful fabrication of biogenic IAA-AgNPs was confirmed by Fourier Transform Infrared Spectrophotometer (FTIR) analysis of IAA which showed absorbance peak at 3434.78 cm-1 due to the N-H stretch of primary amines. Highly resolution Transmission Electron Microscopy (HR-TEM) showed AgNPs coating or capping with IAA in spherical shaped with size ranged from 6.01 to 44.02 nm. Energy dispersive X-ray (EDX) analysis revealed that Ag+ ions were attached to the surface of IAA-AgNPs particles. HR-TEM examination showed cell wall damage of Citrobacter freundii cells after exposure to IAA-AgNPs leading to cell death. In vivo results showed that C. freundii infection of rats induced significant increase in liver and kidney functions and deleterious histopathological alteration in rat's tissues. However, treatment by extracted IAA and IAA-AgNPs could normalize the biochemical and histopathological alterations occurred in infected rats. This is the first study to prove that IAA extracted from Azospirillum brasilense is a hopeful capping agent for NPs which has potential to protect against pathogenic infections, nontoxic and/or safe on rat's metabolisms.


Assuntos
Azospirillum brasilense , Nanopartículas Metálicas , Animais , Azospirillum brasilense/genética , Ácidos Indolacéticos , Nanopartículas Metálicas/toxicidade , RNA Ribossômico 16S , Ratos , Prata
12.
Saudi J Biol Sci ; 28(6): 3284-3293, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34121866

RESUMO

Solid waste management is a serious ecological problem in Saudi Arabia due to rapid industrialization, population growth and urbanization. Recycling and sorting are in their infancy in Saudi Arabia and huge amounts of mixed household and industrial wastes are still dumped without any pre-treatment. Solid waste management techniques such as incineration, pyrolysis and gasification have high investment costs. Composting and vermicomposting of solid organic waste have been considered as an economically viable and sustainable waste management technologies. However, wastes often contain pollutants, such as heavy metals that are toxic to decomposer micro-organisms. Thus, heavy metals are a challenge for the successful biological treatments. Waste may also contain a mixture of organic pollutants that certain microbes, such as micro-algae are known to degrade. The present review paper focuses on understanding the role of vermicomposting as a management tool in mitigating solid organic wastes. It is noteworthy to mention that the microbes also play a pivotal role in the degradation process, wherein the enzymes secreted during the process aid in decomposition of complex molecules into simpler compounds. Also, the extracellular polymeric substance secreted by the earthworm under metal stress serves a source of nutrient for the bacteria to flourish. Henceforth the goal of discussion in present review shows the way forward in using vermicomposting as a novel approach in dealing with solid organic waste.

13.
Chemosphere ; 271: 129532, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33429264

RESUMO

Azo dyes are toxic and recalcitrant environmental pollutants in wastewater and soil in many industrial sites in Asia and Arabic countries. The aim of this study was to find fungal species useful in wastewater treatment and soil remediation efforts. We assessed the ability of different indigenous Aspergillus strains (i.e. A. flavus, A. fumigatus, A. niger and A. terreus) to degrade the azo dyes Acid Blue 29 (AB29), Disperse Red 1 (DR1) and Congo Red (CR). The optimal conditions for dye decolorization by the above-mentioned strains appeared to be as follows: temperature range 30-35 °C, pH 7, glucose as the carbon source (10 g/L), ammonium sulphate as the nitrogen source (1.5 g/L) and 100 mg/L initial dye concentration. The Aspergillus strains decolorized all azo dyes more than 86%. The HPLC and GC-MS analyses confirmed that aniline (retention time 9.0 min), 3-nitroaniline (retention time 15.92 min), 4-nitroanline (retention time 17.81 min), N,N' diethyl-1,4-phenylendiamine (retention time 18.184 min), and benzidine (retention time 15.07 min) were formed as the intermediate metabolites of dye degradation. All Aspergillus strains decolorized 85% of the dyes in synthetic wastewater.


Assuntos
Compostos Azo , Vermelho Congo , Ásia , Biodegradação Ambiental , Corantes , Naftalenos , Níger
14.
Environ Res ; 194: 110672, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33373611

RESUMO

Marine algae have long been explored as food, feed, additives, drugs, and pesticides, yet now the framework is moving towards the algae mediated green synthesis of nanoparticles (NPs). This work is expanding step by step, like algae, are a rich origin of natural compounds. Recently, algae capped and stabilized NPs have picked up far and wide consideration as a less toxic, easy handling, cost effective, eco-friendly, usage in several science fields in nano size, safer to use, and greener method. The natural substance from algae acts as capping or reducing and stabilizing agent in the metal salts to metal, metal oxide, or bimetallic NPs conversion. The NPs using algae could either be intracellular or extracellular relying upon the area of NPs. Among the different scope of algae, reviews are explored in the previous report, still, different NPs using algae and their characterization, mechanism of activity is yet to be summarized. Because of the biocompatibility, good and remarkable physicochemical properties of NPs, the algal biosynthesized NPs have additionally been read for their biomedical applications, which include antibacterial, antioxidant, free radical scavenging, antifungal, anticancer, and biocompatibility properties. In this survey, the reasoning behind the algae mediated biosynthesis of various NPs from different algae origin have been explored. Besides, a piece of knowledge into the component of biosynthesis of NPs from marine algae and their biomedical applications has been summarized.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Antibacterianos , Antioxidantes , Nanopartículas Metálicas/toxicidade , Extratos Vegetais
15.
Future Sci OA ; 6(2): FSO440, 2020 Feb 03.
Artigo em Inglês | MEDLINE | ID: mdl-32025329

RESUMO

Candida albicans has remained the main etiological agent of candidiasis, challenges clinicians with high mortality and morbidity. The emergence of resistance to antifungal drugs, toxicity and lower efficacy have all contributed to an urgent need to develop alternative drugs aiming at novel targets in C. albicans. Targeting the production of virulence factors, which are essential processes for infectious agents, represents an attractive substitute for the development of newer anti-infectives. The present review highlights the recent developments made in the understanding of the pathogenicity of C. albicans. Production of hydrolytic enzymes, morphogenesis and biofilm formation, along with their molecular and metabolic regulation in Candida are discussed with regard to the development of novel antipathogenic drugs against candidiasis.

16.
Mini Rev Med Chem ; 20(5): 418-429, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31161988

RESUMO

BACKGROUND & OBJECTIVE: Quinazolines and their fused systems are noteworthy in pharmaceutical chemistry due to their wide range of biological activities. METHODS: A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol. RESULTS: The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of the preparation and design of the above mentioned compounds has been shown to be clear in the results of their antimicrobial activity which revealed that some derivatives have potent activity exceeding or similar to the activity of the reference drugs. CONCLUSION: The insertion of triazole or thiazole moieties to be fused with quinazoline ring helps to enhance its antimicrobial activity.


Assuntos
Quinazolinas/química , Quinazolinas/síntese química , Quinazolinas/farmacologia , Tiazepinas/química , Tiazepinas/síntese química , Tiazepinas/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Azóis/síntese química , Azóis/química , Azóis/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
17.
Mini Rev Med Chem ; 19(15): 1276-1290, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30864524

RESUMO

BACKGROUND: Bis-heterocycles especially those containing pyrazole moiety display much better antibacterial activity than mono heterocycles. OBJECTIVE: Herein, we synthesised a series of new bis-pyrazoles and investigated their antimicrobial agents. METHODS: A novel series of bis-pyrazole derivatives have been synthesized in good yield by coupling reaction of cyanoacetic acid {4-[(2-cyano-acetyl)-hydrazonomethyl]-benzylidene}-hydrazide with a number of diazonium salts of aromatic amines in DMF in the presence of NaOH. Refluxing of the produced hydrazones with hydrazine-hydrate in ethanolic solution afforded the respective bis-pyrazoles. On the other hand, the reaction of bis(cyanoacetic acid hydrazide) derivative with a diversity of hydrazonoyl chlorides in dioxane under reflux gave bis-pyrazoles. RESULTS: The structures of all the products were discussed and assured from all possible spectral data as well as for the elemental analysis. In addition, the results of the antimicrobial activity examination of selected derivatives revealed a high strength of some tested compounds compared to standard bactericides and fungicides utilized. Molecular docking of the newly synthesized compounds into the Enoyl ACP reductase active site supported the in vitro antimicrobial activity. All the tested compounds could fit in the enzyme binding pocket with significant binding affinities (-7.040 to -9.141 Kcal/mol). CONCLUSION: The good results of the antimicrobial examination of the newly synthesized bis-pyrazoles comprise the considerable evidence of the importance of bis-heterocyclic compounds which encourages us to continue designing and synthesising a novel series with potent biological activity in the future.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Pirazóis/síntese química , Pirazóis/farmacologia , Antibacterianos/química , Antifúngicos/química , Aspergillus niger/efeitos dos fármacos , Relação Dose-Resposta a Droga , Geotrichum/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Estrutura Molecular , Pirazóis/química , Relação Estrutura-Atividade
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