SYNTHESIS AND IN-VITRO CARDIOVASCULAR ACTIVITY OF 4-ARYL-2,3,3A,4-TETRAHYDRO-1H-PYRROLO[2,1-C][1,4]BENZOTHIAZIN-1-ONES AND 7-ACETOXY-6-PHENYL-7A,8,9,10-TETRAHYDROPYRROLO[2,1-D][1,5]BENZOTHIAZEPIN-10-ONE

被引：8

作者：

CAMPIANI, G

GAROFALO, A

FIORINI, I

NACCI, V

BOTTA, M

TAFI, A

CHIARINI, A

BUDRIESI, R

BRUNI, G

ROMEO, MR

机构：

[1] UNIV SIENA,DIPARTIMENTO FARM CHIM TECNOL,BANCHI SOTTO 55,I-53100 SIENA,ITALY

[2] UNIV BOLOGNA,DIPARTIMENTO SCI FARMACEUT,I-40126 BOLOGNA,ITALY

[3] UNIV SIENA,IST FARM,I-53100 SIENA,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)80337-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and die pharmacological characterization of novel heterocyclic systems 1 and 2 is described. On radioreceptor assay la showed higher affinity for Calcium Channel Receptors (CCRs) and in functional studies higher potency and efficacy as negative inotropic agent than Diltiazem, without relevant calcium antagonist activity on vascular smooth muscle, revealing a clear-cut selectivity for cardiac over vascular tissue.

引用

页码：1235 / 1240

页数：6

共 18 条

[1] LONG-ACTING DIHYDROPYRIDINE CALCIUM-ANTAGONISTS .4. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS FOR A SERIES OF BASIC AND NONBASIC DERIVATIVES OF 2-[(2-AMINOETHOXY)METHYL]-1,4-DIHYDROPYRIDINE CALCIUM-ANTAGONISTS [J].