SYNTHESIS AND IN-VITRO CARDIOVASCULAR ACTIVITY OF TRAHYDRO-1H-PYRROLO[2,1-C][1,4]BENZOTHIAZIN-1-ONES AND TETRAHYDROPYRROLO[2,1-D][1,5]BENZOTHIAZEPIN-10-ONE

Authors
CAMPIANI G GAROFALO A FIORINI I NACCI V BOTTA M TAFI A CHIARINI A BUDRIESI R BRUNI G ROMEO MR
Citation
G. Campiani et al., SYNTHESIS AND IN-VITRO CARDIOVASCULAR ACTIVITY OF TRAHYDRO-1H-PYRROLO[2,1-C][1,4]BENZOTHIAZIN-1-ONES AND TETRAHYDROPYRROLO[2,1-D][1,5]BENZOTHIAZEPIN-10-ONE, Bioorganic & medicinal chemistry letters, 4(10), 1994, pp. 1235-1240
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
10
Year of publication
1994
Pages
1235 - 1240
Database
ISI
SICI code
0960-894X(1994)4:10<1235:SAICAO>2.0.ZU;2-9
Abstract
The synthesis and die pharmacological characterization of novel hetero cyclic 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 sm ooth muscle, revealing a clear-cut selectivity for cardiac over vascul ar tissue.