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1.
Farmaco ; 56(8): 549-54, 2001 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-11601639

RESUMO

9,10-Anthracenedione derivatives are known to exhibit a quite potent anticancer activity. It has also been reported that these compounds can be effectively employed in both antibacterial and antitrypanosomal therapy. Anthraquinones also exhibit some undesirable side effects, like cardiotoxicity. So many interactions seem to demonstrate that 9,10-anthracenediones strongly interact with a number of biological sites. In this paper we wish to report on the synthesis and the pharmaceutical activity of some newly synthesised derivatives containing the anthraquinone pharmacophore.


Assuntos
Antraquinonas/síntese química , Anti-Infecciosos/síntese química , Antraquinonas/farmacologia , Anti-Infecciosos/farmacologia , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade
2.
Farmaco ; 55(2): 93-8, 2000 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-10782378

RESUMO

Arylidenimidazoles bearing a thioethereal function in the position 2 of the imidazole ring show good antimicrobial activity. We now report on the synthesis and the biological properties of some novel arylidenisothiosemicarbazones, structurally related to the arylideneiminoimidazoles of which they can be considered the linear precursors. Particular attention has been put on the influence of structural modifications on the biological activity.


Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Tiossemicarbazonas/síntese química , Tiossemicarbazonas/farmacologia , Anti-Infecciosos/química , Química Farmacêutica , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade , Tiossemicarbazonas/química
3.
Farmaco ; 59(12): 945-52, 2004 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-15598429

RESUMO

The synthesis of some aroylisothiosemicarbazides was accomplished and their biological activity against bacteria, fungi, and mycobacteria was investigated. Different synthetic pathways were followed according to the kind of substituents that were introduced on both the aroyl ring and the sulfur atom. Anti-bacterial activity was measured against Staphylococcus aureus, S. epidermidis, Streptococcus agalactiae and S. faecalis, Escherichia coli, and Salmonella typhi, while antifungal activity was evaluated against C. albicans. Two species, Mycobacterium tuberculosis H37RV and Mycobacterium avium ATCC19421, were employed to evaluate antimycobacterial activity.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Semicarbazidas/síntese química , Semicarbazidas/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Testes de Sensibilidade Microbiana/métodos
4.
Farmaco ; 57(10): 809-17, 2002 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-12420876

RESUMO

It is known that some derivatives of both thiourea and thiosemicarbazide exhibit potent anti-microbial activity. In order to investigate the effects on the biological properties of structural modifications of such structures, we have synthesised and studied some arylidenisothiosemicarbazones. In this paper we report on the synthesis and structure-activity relationships of some isothiosemicarbazones, where the arylidene group has been replaced with a cycloalkyl group and the sulfur atom has been either differently substituted or enclosed in a thiazole ring.


Assuntos
Anti-Infecciosos/farmacologia , Tiossemicarbazonas/química , Tiossemicarbazonas/farmacologia , Animais , Antibacterianos , Anti-Infecciosos/síntese química , Chlorocebus aethiops , Fungos/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Interações Hidrofóbicas e Hidrofílicas , Testes de Sensibilidade Microbiana , Espectrometria de Massas por Ionização por Electrospray , Relação Estrutura-Atividade , Células Vero/efeitos dos fármacos
5.
Farmaco ; 58(9): 951-9, 2003 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-13679191

RESUMO

Several arylideneisothiosemicarbazones and arylidenehydrazothiazoles have been synthesised to obtain new antimicrobial agents. Their activity against both bacteria and fungi has been tested and some interesting informations about their biological activity have been obtained.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Tiossemicarbazonas/farmacologia , Antibacterianos/química , Antifúngicos/química , Desenho de Fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade , Tiossemicarbazonas/química , Leveduras/efeitos dos fármacos
6.
Farmaco ; 53(10-11): 698-708, 1998.
Artigo em Inglês | MEDLINE | ID: mdl-10205857

RESUMO

In this study some cycloalkyl-3-(N-substituted carbamoyl)-1-phenylpyrazoles have been synthesized in order to screen their capability to inhibit human cyclooxygenase. The synthetic pathway is based on the well known property of nitrilimines to undergo 1,3-dipolar cycloaddition reactions. The structures of all the synthesized compounds have been elucidated by means of both analytical and spectroscopic methods.


Assuntos
Inibidores de Ciclo-Oxigenase/síntese química , Pirazóis/síntese química , Inibidores de Ciclo-Oxigenase/química , Humanos , Espectroscopia de Ressonância Magnética , Pirazóis/química , Estereoisomerismo
7.
Int J Occup Saf Ergon ; 7(3): 363-70, 2001.
Artigo em Inglês | MEDLINE | ID: mdl-11543704

RESUMO

This work proposes to show the experience of posture training accomplished in the Paraíba State Telecommunication Company, using the knowledge of the Back School. The sample was composed of 12 operators, employees of the company, representing 31% of this population. The model applied in TELPA (Paraíba Telecommunication Company, Brazil) was based on the models of Sherbrooke, Canada, and of the School of Posture of Paraìba Federal University. Fifty-eight point four percent of participants showed a reduction of column pain, 25% improved the quality of the rest and the received training was considered enough for the learning of correct postures at work in 75% of the cases. The whole population approved of the training, and 83.3% of the cases considered that this training influenced their lives very positively.


Assuntos
Dor nas Costas/prevenção & controle , Modalidades de Fisioterapia/métodos , Postura/fisiologia , Telecomunicações , Adulto , Brasil , Feminino , Humanos , Masculino , Resultado do Tratamento
8.
Eur J Med Chem ; 45(10): 4490-8, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-20702005

RESUMO

Some differently substituted 3-aryl-4,5-dihydropyrazoles-1-carbothioamides have been synthesised with the aim to investigate their monoamine oxidase inhibitory activity. The chemical structures of the compounds have been characterized by means of their IR, (1)H NMR, (13)C NMR spectroscopic data and elemental analyses. All the active compounds showed a selective activity towards the B isoform of the enzyme, regardless of the substitution on the heterocyclic ring. The inhibition of the enzymatic activity was measured on human recombinant MAO isoforms, expressed in baculovirus infected BTI insect cells. Docking experiments were carried out with the aim to rationalize the mechanism of inhibition of the most active and selective compound.


Assuntos
Inibidores da Monoaminoxidase/química , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/metabolismo , Pirazóis/química , Pirazóis/farmacologia , Tioamidas/química , Tioamidas/farmacologia , Animais , Linhagem Celular , Humanos , Insetos , Modelos Moleculares , Inibidores da Monoaminoxidase/síntese química , Ligação Proteica , Pirazóis/síntese química , Proteínas Recombinantes/antagonistas & inibidores , Proteínas Recombinantes/metabolismo , Relação Estrutura-Atividade , Tioamidas/síntese química
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