DIHYDROPYRIMIDINE CALCIUM-CHANNEL BLOCKERS 51 - BICYCLIC DIHYDROPYRIMIDINES AS POTENT MIMICS OF DIHYDROPYRIDINES

被引：81

作者：

ATWAL, KS

MORELAND, S

机构：

[1] Bristol-Myers Squibb, Pharmaceutical Research Institute, Princeton, NJ 08543-4000

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(01)80810-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Bicyclic dihydropyrimidines 3 imitating the in vitro potency of dihydropyridine calcium channel blockers (e.g., nifedipine 2) are described. Structure-activity studies show a pyrazole ring can effectively mimic the combined effect of N3-substituent (R3) and C2-hetero atom (X) of monocyclic dihydropyrimidines 1. These results support our previous hypothesis about the requirement of a vinylogous urethane for calcium channel blocking activity and a nonspecific role for the N3-substituent and C2-hetero atom (X) of 1.

引用

页码：291 / 294

页数：4

共 7 条

[1] DIHYDROPYRIMIDINE CALCIUM-CHANNEL BLOCKERS .3. 3-CARBAMOYL-4-ARYL-1,2,3,4-TETRAHYDRO-6-METHYL-5-PYRIMIDINECARBOXYLIC ACID-ESTERS AS ORALLY EFFECTIVE ANTIHYPERTENSIVE AGENTS [J].