SYNTHESIS AND CALCIUM ANTAGONISTIC ACTIVITY OF SOME NEW 2-THIOXO-1,2,3,4-TETRAHYDROPYRIMIDINE DERIVATIVES

被引：27
|
作者：
ERTAN, M
BALKAN, A
SARAC, S
UMA, S
RENAUD, JF
ROLLAD, Y
机构：
[1] FONDAX ACTAM & CIE,RECH SERVIER GRP,PUTEAUX,FRANCE
[2] HACETTEPE UNIV,FAC PHARM,DEPT PHARMACOL,ANKARA,TURKEY
来源：
ARCHIV DER PHARMAZIE | 1991年 / 324卷 / 03期
关键词：
D O I：
10.1002/ardp.19913240302
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 1,2,3,4-tetrahydro-6-methyl-4-(substituted phenyl)-2-thioxo-5-pyrimidinecarboxylic acid methyl esters were synthesized by condensing thiourea with methyl acetoacetate and nonsubstituted or differently substituted benzaldehydes in absol. ethanol using HCl as a catalyst according to the Biginelli reaction. The structures of the compounds were confirmed by elemental and spectroscopic analysis. The compounds were evaluated for their calcium antagonistic activity on the basis of their potency in inhibiting [H-3] PN 200-110 binding on microsomes obtained from rat skeletal muscle.
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页码：135 / 139
页数：5
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