SYNTHESIS AND QSAR IN 2,3,6,8-SUBSTITUTED 1,3-QUINAZOLIN-4(4H)-ONES AS POTENTIAL ANTHELMINTICS

被引:0
|
作者
SRIVASTAVA, B
SHUKLA, JS
PRABHAKAR, YS
SAXENA, AK
机构
[1] UNIV LUCKNOW, DEPT CHEM, LUCKNOW 226007, UTTAR PRADESH, INDIA
[2] CENT DRUG RES INST, DIV MED CHEM, LUCKNOW 226001, UTTAR PRADESH, INDIA
关键词
D O I
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中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
6, 8-Disubstituted-3-aryl-2-[3-mercapto-4-aryl)-1, 3, 4-triazole-5-ylmethylthio]-1, 3-quinazolin-4-(4H)-ones (6) and 2-methyl/phenyl-3-(4-substituted phenylimino-4-oxothiazolidine-3-ylphenyl)-6,8-disubstituted-1,3-quinazolin-4(4H)-ones (11) have been synthesised and evaluated for their anthelmintic activity against H. nana in mice, A. ceylanicum in hamsters and N. brasiliensis in rats. None of these compounds shows activity against H. nana. The QSAR studies of these compounds have been carried out in terms of structural and physico-chemical parameters where positive contribution of substituents present at 6- and 8-positions and effect of hydrophobicity at 3-position have been found to influence the activity.
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页码:332 / 339
页数:8
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