INOTROPIC 2-ARYLIMIDAZOL[1,2-A]PYRIMIDINES

被引：8

作者：

BARRACLOUGH, P

BLACK, JW

CAMBRIDGE, D

CAPON, E

COX, MR

FIRMIN, D

GERSKOWITCH, VP

GILES, H

GLEN, RC

HILL, AP

HULL, RAD

IYER, R

KETTLE, D

KING, WR

NOBBS, MS

RANDALL, P

SKONE, P

SMITH, S

VINE, SJ

WHARTON, CJ

WHITING, MV

机构：

[1] WELLCOME RES LABS,DEPT PHARMACOL,BECKENHAM BR3 3BS,KENT,ENGLAND

[2] WELLCOME RES LABS,DEPT PHYS SCI,BECKENHAM BR3 3BS,KENT,ENGLAND

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 03期

关键词：

CARDIOTONICS; INOTROPES; IMIDAZOPYRIMIDINE; SULMAZOLE; ISOMAZOLE;

D O I：

10.1016/0223-5234(92)90004-K

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-arylimidazo[1,2-a]pyrimidines has been prepared and evaluated for inotropic activity. Three of these heterocycles. ether 19, sulphide 21 and mesylate 24 displayed more potent inotropic effects in vitro than isomazole. The in vivo inotropic potencies of 4'-mesylate 24 and 4'-carboxamido analogue 23 were similar to those of isomazole and sulmazole respectively. The effects of some 'A' and 'C' ring substituents on the inotropic activities of the imidazo[1,2-a]pyrimidines were different from those on the imidazopyridines. Nevertheless the inotropic potencies of several imidazo[1.2-a]pyrimidines were closer to those of their 1H-imidazo[4,5-b]pyridine isomers than to those of the corresponding isomazole analogues. Structure-activity relationships are discussed in detail.

引用

页码：207 / 217

页数：11

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