CYCLOPENTANESPIRO-3H-DIHYDRO-PYRIMIDINONES AS ANGIOTENSIN-II AT(1) RECEPTOR ANTAGONISTS

Authors
BERNHART CA HAUDRICOURT FB ASSENS JL GOUGAT J LACOUR C ROCCON A CAZAUBON C BRELIERE JC LEFUR G NISATO D
Citation
Ca. Bernhart et al., CYCLOPENTANESPIRO-3H-DIHYDRO-PYRIMIDINONES AS ANGIOTENSIN-II AT(1) RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 157-162
Citations number
4
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
157 - 162
Database
ISI
SICI code
0960-894X(1994)4:1<157:CAAAR>2.0.ZU;2-L
Abstract
A novel series of substituted H-3-dihydro-pyrimidinones, homologues of SR 47436, was identified as AT(1) receptor antagonists. The best comp ounds showed high affinity for the AT(1) receptor (rat liver membrane preparation) with IC50's in the nanomolar range. Active p.o. in rats i n an AII infused model, they are inactive in cynomolgus monkeys.