Synthesis of novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest: a 3D-QSAR study on their cytotoxicity

被引：0
作者：
B. R. Prashantha Kumar
Pankaj Masih
E. Karthikeyan
Ankur Bansal
Pottekad Suja
机构：
[1] JSS College of Pharmacy,Department of Pharmaceutical Chemistry
[2] JSS College of Pharmacy,Department of Biotechnology
来源：
Medicinal Chemistry Research | 2010年 / 19卷
关键词：
Dihydropyrimidines; Dihydropyridines; CoMFA; Cytotoxicity;
D O I：
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学科分类号：
摘要：
We report a library consisting of some novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest as well as their synthesis and analysis. The important steps in the synthetic part were found to be Hantzsch and Biginelli multicomponent reactions. The synthesized compounds were screened for their in vitro antibacterial activity against two gram-positive bacteria: Staphylococcus aureus and Bacillus subtilis. The title compounds did not exhibit potential antibacterial activity. Furthermore, compounds were subjected to in vitro cytotoxicity against Vero cells. Compounds exhibited weak, moderate, or high cytotoxicity. Compounds 4a, 4b, 4c, 4f, 4g, 4h, 4i, 7i, 7l, 7m, and 7r exhibited potential cytotoxicity. CoMFA study has resulted in the identification of structural features contributing toward their cytotoxicity.
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页码：344 / 363
页数：19
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