Synthesis and antimicrobial activity of novel pyrazole, pyrazoline, pyrazolinone and pyrazolidinedione derivatives of benzimidazole.
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.
Soliman
R
R
Pharmaceutical Chemistry Department, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
Habib
N S
NS
Ashour
F A
FA
el-Taiebi
M
M
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D001562:Benzimidazoles; D007202:Indicators and Reagents; D011720:Pyrazoles