RESUMO
Four novel series of pyrazolylbenzimidazole derivatives have been prepared, namely 2-[(1-substituted phenyl-3,5-dimethyl-4-pyrazolyl)methyl]benzimidazole 5a-d 2-[(1-substituted phenyl-3-methyl-5-oxo-4,5-dihydro-4-pyrazolyl-4-yl)methyl]benzimidazoles 6a-d; 2-[(1-substituted phenyl-3,5-dioxopyrazolidin-4-yl)methyl]benzimidazoles 7a-d and 2-[(4-(1-phenyl-5-aryl-4,5-dihydro-3-pyrazolyl)phenylaminoacetyl]thio- methyl)-benzimidazoles 12a-e. The antimicrobial testing of the prepared compounds was performed using Escherichia Coli (NCTC 5933) as Gram-negative bacteria, Staphylococcus aureus (NCTC 4163) as gram-positive bacteria and Candida albicans (NCTC 5310) as yeast like fungi. The most potent compound was the pyrazolone 6a which exhibits interesting antibacterial activity against the gram-negative bacteria E. coli.
Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Pirazóis/síntese química , Pirazóis/farmacologia , Antibacterianos , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Indicadores e Reagentes , Testes de Sensibilidade MicrobianaRESUMO
Three novel series of benzimidazole derivatives namely 6-substituted 3-[1-(2-alkyl-1 H-benzimidazolyl)methyl]-1,2,4-triazolo[3,4-b][1,3,4] thiadiazoles 5a-h, 6-substituted 3-[1-(2-alkyl-1H-benzimidazolyl)methyl]-7H-1,2,4 -triazolo[3,4-b]-[1,3,4]thiadiazines 6a-j and 6-thioxo-3-[1-(2-alkyl-1H-benzimidazolyl)methyl]-5,6-dihydro-1,2,4 -triazolo[3,4-b][1,3,4]-thiadiazoles 7a, b have been prepared by cyclization of the key intermediate 1-[(4-amino-5-mercapto-4 H-1,2,4-triazol-3-yl)methyl]-2-alkyl-1 H-benzimidazoles 3a, b. Furthermore, 1-[(4-arylideneamino-5-mercapto- 4H-1,2,4-triazol-3-yl)-methyl]-2-alkyl- 1 H-benzimidazoles 4a-h have been prepared and some of them were cyclized to 6-substituted 3-[1-(2-alkyl-1H-benzimidazolyl)methyl]-1,2,4-triazolo [3,4-b][1,3,4]thiadiazoles 5d, h using thionyl chloride. The prepared compounds were tested for antimicrobial activity in vitro; they showed moderate activity.
Assuntos
Anti-Infecciosos/síntese química , Bactérias/efeitos dos fármacos , Benzimidazóis/síntese química , Triazóis/síntese química , Antibacterianos , Anti-Infecciosos/farmacologia , Benzimidazóis/farmacologia , Candida albicans/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Staphylococcus aureus/efeitos dos fármacos , Triazóis/farmacologiaRESUMO
Three novel series of oxadiazolylbenzimidazole derivatives have been prepared, namely 1-[(2-alkylthio or aralkylthio-1,3,4-oxadiazol-5-yl)methyl]-2-alkyl-1 H-benzimidazoles 3a-f; 1-[(3-substituted aminomethyl-2-thioxo-2,3-dihydro-1,3,4-oxadiazol-5-yl)methyl ]-2-alkyl-1 H-benzimidazoles 4a-f and 1-[(2-substituted amino-1,3,4-oxidiazol-5-yl)methyl]-2-alkyl-1 H-benzimidazoles 6a-j. The antimicrobial testing of the prepared compounds was performed, some of them showed week activity.
