Syntheses and QSAR studies of 5-imidazolinone derivatives as potential antibacterial agents

Abstract

Several 2-[(4-arylmethylene-5-oxo-2-phenyl-1-imidazolinyl)amino]-N-(4-nitropheny l)acetamides 1,2-[(4-arylmethylene-5-oxo-2-phenyl-1-imidazolinyl)amino]-N-benzy lacetamides 2, 2-(4-chlorophenyl)-N-(4-arylmethylene-5-oxo-2- phenyl-1-imidazolinyl) acetamides <b>3</b> and N-(4-arylmethylene-5-oxo-2-phenyl-1-imidazolinyl)-N¹-(2,6-dimethylphenyl)thioureas <b>4</b> have been synthesised and evaluated for their antibacterial act ivity against gram (+)ve <i>S</i>. <i>aureus </i>and gram (-)ve <i>E</i>. <i>Coli</i> bacteria. Most of the compounds have shown moderate to good activity against gram (+)ve and gram (-)ve bacteria.

Correlation studies between the two models of anti bacterial screening have established the complementarity between the two models. The QSAR studies of these compounds have been carried out in terms of structural and physicochemical parameters where positive contribution by bulky lipophilic groups with increased electropositive character in the aryl part at 4-position of imidazolinones <b>1</b> has been observed.