QSAR modeling of synthesized 3-(1,3-benzothiazol-2-yl) 2-phenyl quinazolin-4(3H)-ones as potent antibacterial agents

被引:0
作者
Pratibha Sharma
Ashok Kumar
Prerna Kumari
Jitendra Singh
M. P. Kaushik
机构
[1] Devi Ahilya University,School of Chemical Sciences
[2] Defense Research and Development Establishment,undefined
来源
Medicinal Chemistry Research | 2012年 / 21卷
关键词
Quinazoline-4(3; )-ones; Benzothiazole; Quantitative structure–activity relationship; Antibacterial activity;
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摘要
Present communication elicits the designing and synthesis of 3-(1,3-benzothiazol-2-yl) 2-phenyl quinazolin-4(3H)-ones as potential antibacterial agents. A number of substituted 2-amino benzothiazoles, 2-amino-5-[(E)-phenyl diazenyl] benzoic acid, and 2-phenyl-4H benzo[d] [1,3] oxazin-4-one were synthesized as the precursor substrates. The compounds were synthesized in excellent yields and the structures were corroborated on the basis of IR, 1H NMR, Mass, and elemental analysis data. These compounds were screened in vitro for their antibacterial activity against a representative panel of Gram positive and Gram negative bacteria and models were generated through quantitative structure–activity relationship (QSAR).The activity contributions due to structural and substituent effects were determined using sequential regression procedure. The antimicrobial assay data show that the synthesized compounds are found to manifest profound antimicrobial activity.
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页码:1136 / 1148
页数:12
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