RESUMO
New N-(5-methylisoxazol-3-yl)-2 or 3 or 4-(phenoxyacetamido)benzamides 6a-t were synthesized and tested for their in vitro antimicrobial activity against gram positive (Staphylococcus aureus ATCC 25923) and gram negative (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853) bacteria as well as fungi (Candida albicans ATCC 10231, Candida tropicalis ATCC 13803 and Cryptococcus neoformans ATCC 90112). Compounds 6 were devoid of antibacterial as well as antifungal activities at maximum tested concentrations of 50 micrograms/ml for bacteria and 100 micrograms/ml for yeast.
Assuntos
Acetamidas/síntese química , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Éteres Fenílicos/síntese química , Acetamidas/farmacologia , Antibacterianos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Éteres Fenílicos/farmacologiaRESUMO
Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl] -1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3 alpha-HSD, but no correlation was observed with the paw edema inhibition values. The compounds proved to possess marginal or no ulcerogenic effect, as well as low systemic toxicity.
Assuntos
3-Hidroxiesteroide Desidrogenases/antagonistas & inibidores , Analgésicos/síntese química , Anti-Inflamatórios/síntese química , Inibidores Enzimáticos/síntese química , Pirazóis/síntese química , 3-alfa-Hidroxiesteroide Desidrogenase (B-Específica) , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Inibidores Enzimáticos/farmacologia , Masculino , Camundongos , Pirazóis/farmacologia , RatosAssuntos
3-Hidroxiesteroide Desidrogenases/antagonistas & inibidores , Inibidores Enzimáticos/síntese química , Pirazóis/síntese química , Pirimidinonas/síntese química , Inibidores Enzimáticos/farmacologia , Espectroscopia de Ressonância Magnética , Pirazóis/farmacologia , Pirimidinonas/farmacologia , Espectrofotometria InfravermelhoRESUMO
The synthesis of some pyrazolo [4,3-e] [1,4] diazepin-5,8-diones has been accomplished starting from the readily available 1-ethyl-3-methyl-4-nitro-5-pyrazolecarbonylchloride and the appropriate alpha-aminoesthers, 2a, b, c. The catalytic reduction of the obtained 3a, b, c gave the products 4a, b, c which were, in turn, cyclized into the title compounds 5a, b, c. The intermediates of type 3 and 4 and the pyrazolo-diazepin-diones 5 were tested in vitro for their antimicrobial activity.
Assuntos
Antibacterianos/síntese química , Azepinas/síntese química , Bactérias/efeitos dos fármacos , Antibacterianos/farmacologia , Azepinas/farmacologia , Testes de Sensibilidade MicrobianaAssuntos
Azepinas/síntese química , Fármacos do Sistema Nervoso Central/síntese química , Pirazóis/síntese química , Animais , Azepinas/farmacologia , Comportamento Animal/efeitos dos fármacos , Fármacos do Sistema Nervoso Central/farmacologia , Conflito Psicológico , Discriminação Psicológica/efeitos dos fármacos , Comportamento de Ingestão de Líquido/efeitos dos fármacos , Masculino , Atividade Motora/efeitos dos fármacos , Pentobarbital/farmacologia , Pentilenotetrazol/farmacologia , Pirazóis/farmacologia , Ratos , Ratos Endogâmicos , Percepção do Tempo/efeitos dos fármacosRESUMO
New imidazolylpyrazoles were synthesized and tested for antimicrobial activities. The compounds did not show any significant activity.
Assuntos
Anti-Infecciosos/síntese química , Imidazóis/síntese química , Pirazóis/síntese química , Antibacterianos , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Imidazóis/farmacologia , Testes de Sensibilidade Microbiana , Pirazóis/farmacologiaRESUMO
The synthesis of 1-phenyl-5,8-dimethyl-1,4,5,6,7,8-hexahydro-pyrazolo[3,4-e][1,4] diazepin-4,7-dione and of 1-phenyl-3,5,8-trimethyl-1,4,5,6,7,8-hexahydro-pyrazolo[3,4-e] [1,4]diazepin-4,7-dione is described. These compounds exhibit activity on CNS in animals.