title: Antibacterial activity of synthesized 2,4,5-trisubstituted imidazole derivatives.
abstract: 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.
authors.affiliation: Division of Biochemical Science, National Chemical Laboratory, Pune 411 008, India.
authors.forename: Mohd Sajid
authors.initials: MS
authors.lastname: Khan
authors.forename: Shafi Ahmad
authors.initials: SA
authors.lastname: Siddiqui
authors.forename: Mohammad Shaik Rafi Ahmad
authors.initials: MS
authors.lastname: Siddiqui
authors.forename: Usha
authors.initials: U
authors.lastname: Goswami
authors.forename: Kumar Venkatraman
authors.initials: KV
authors.lastname: Srinivasan
authors.forename: Muhammad Islam
authors.initials: MI
authors.lastname: Khan
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D007093:Imidazoles; D010636:Phenols