Antibacterial activity of synthesized 2,4,5-trisubstituted imidazole derivatives.
Some novel chemically synthesized 2,4,5-trisubstituted imidazoles from aryl aldehydes and 1,2-diketones or alpha-hydroxyketone were screened against eight different human pathogenic bacteria and fungi. Seven compounds were found to be active against different bacteria. These compounds showed variation in activity and were found to be active against Gram-positive as well as Gram-negative bacteria. Compound 4-(4,5-diphenyl-1H-imidazol-2-yl)-phenol, 3d was the only compound which showed activity against Klebsiella pneumoniae while rest of the compounds did not show significant activity against this micro-organism. Minimum inhibitory concentrations of the compounds were in the range of 0.50 to 6.1 microg/mL and minimum bactericidal concentration ranges from 1.11 to 12.9 microg/mL. The candidature of active compounds to be an effective and novel drug was examined based on Lipinski's rule of Five which explained ClogP, LogS, H-bond acceptors, H-Bond donors and rotational bonds. Compounds 3a-d and 3f satisfies Lipinski's rule of Five and could be proposed as potent new antibacterial drugs.
Khan
Mohd Sajid
MS
Division of Biochemical Science, National Chemical Laboratory, Pune 411 008, India.
Siddiqui
Shafi Ahmad
SA
Siddiqui
Mohammad Shaik Rafi Ahmad
MS
Goswami
Usha
U
Srinivasan
Kumar Venkatraman
KV
Khan
Muhammad Islam
MI
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007711:Klebsiella pneumoniae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D010636:Phenols / Q000138:chemical synthesis / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D007093:Imidazoles; D010636:Phenols