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Antibacterial activity of synthesized 2,4,5-trisubstituted imidazole derivatives

DRS at CSIR-National Institute of Oceanography

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Title Antibacterial activity of synthesized 2,4,5-trisubstituted imidazole derivatives
 
Creator Khan, M.S.
Siddiqui, S.A.
Siddiqui, M.S.R.A.
Goswami, U.
Srinivasan, K.V.
Khan, M.I.
 
Subject Antibacterial activity
pathogenic bacteria
 
Description Some novel chemically synthesized 2,4,5-trisubstituted imidazoles from aryl aldehydes and 1,2-diketones or a-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 mu g/mL and minimum bactericidal concentration ranges from 1.11 to 12.9 mu g/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 3aûd and 3f satisfies Lipinski's rule of Five and could be proposed as potent new antibacterial drugs
 
Date 2008-10-17T15:40:32Z
2008-10-17T15:40:32Z
2008
 
Type Journal Article
 
Identifier Chemical biology & drug design, Vol.72; 197-204p.
http://drs.nio.org/drs/handle/2264/1471
 
Language en
 
Rights Copyright [2008]. All efforts have been made to respect the copyright to the best of our
knowledge. Inadvertent omissions, if brought to our notice, stand for correction and withdrawal of document from this repository.
 
Publisher Blackwell Munksgaard