SYNTHESIS AND IN-VITRO EVALUATION OF FUSED-RING HETEROCYCLE-CONTAINING ANGIOTENSIN-II ANTAGONISTS

Authors
ZYDOWSKY TM WINN M DE B CONDON SL ALTENBACH RJ BASHA FZ BOYD SA BUCKNER SA HANCOCK AA LEE JY MANTEI RA NOVOSAD EI SORENSEN BK TASKER AS SHIOSAKI K KERKMAN DJ OPGENORTH TJ DEBERNARDIS JF
Citation
Tm. Zydowsky et al., SYNTHESIS AND IN-VITRO EVALUATION OF FUSED-RING HETEROCYCLE-CONTAINING ANGIOTENSIN-II ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 173-176
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
1
Year of publication
1994
Pages
173 - 176
Database
ISI
SICI code
0960-894X(1994)4:1<173:SAIEOF>2.0.ZU;2-C
Abstract
Fused ring heterocyclic analogs of A-81080 (pA(2)=9.9) were synthesize d and their activities in the rabbit aorta in vitro assay were measure d. The best compounds (pA(2)=8.6) in series 1 had R(1)=Et, R(2)=H, W=Z =C-H, and Y=C-Ome or C-COOH. In series 2, the best compound (pA(2)=8.3 ) had R(1)=Et, R(2)=H, W=N-Me, X=C-H, and Y=N.