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Title: Synthesis and QSAR studies of 4-oxo-thiazolidines and 2-oxo-azetidines as potential antibacterial agents
Authors: Desai, N C
Shah, M D
Bhavsar, A M
Keywords: 4-Oxo-thiazolidines
Antibacterial activity
Linear free energy relationship (LFER)
QSAR study
Issue Date: Jul-2008
Publisher: CSIR
Abstract: Several 2-(4-chlorophenyl)-N-(4-oxo-2-aryl(l,3,thiazolidin-3-yl))acetamides 2, N-[3-chloro-4-(2-aryl)-2-oxo-azetidinyl]-2-(4-chlorophenyl)acetamides 3, N-(4-oxo-2-aryl(1,3,-thiadiazolidin-3-yl){4-[5-oxo-2-phenyl-4-(phenylmethylene) (2-imidazolinyl)phenyl}carboxamides 7 and N-(3-chloro-2-oxo-4-arylazetidinyl){4-[5-oxo-2-phenyl-4-(phenylmethylene)(2-imidazolinyl)] phenyl}carboxamides 8 have been synthesized and evaluated for their antibacterial activity against gram +ve and gram -ve bacteria i.e. S. aureus and E. coli. Most of the compounds are showed moderate to good activity against gram +ve and gram -ve bacteria. The QSAR studies of these compounds have been carried out in terms of structural and physicochemical parameters where positive contribution of substituents present at position-3 of N-[3-chloro-4-(2-aryl)-2-oxo-azetidinyl]-2-(4-chlorophenyl)acetamides with bulkier group indicating increase in hydrophobicity or steric bulk character.
Page(s): 1135-1144
ISSN: 0376-4699
Source:IJC-B Vol.47B(07) [July 2008]

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