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

摘要

Several 2-[(4-arylmethylene-5-oxo-2-phenyl-1-imidazolinyl)amino]-N-(4-nitrophenyl)acetamides 1,2-[(4-arylmethylene-5-oxo-2-phenyl-1-imidazolinyl)amino]-N-benzylacetamides 2,2-(4-chlorophenyl)-N-(4-arylmethylene-5-oxo-2-phenyl-1- imidazolinyl)acetamides 3 and N-(4-arylmethylene-5-oxo-2-phenyl-1-imidazolinyl)-N~1-(2,6-dimethylphenyl)thioureas 4 have been synthesised and evaluated for their antibacterial activity against gram (+) ve S.aureus and gram(-)ve E.coli 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 antibacterial 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 1 has been observed.