Cyclopentanespiro-3H-dihydro-pyrimidinones as Angiotensin II AT1 receptor antagonists

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

A novel series of substituted 3Hdihydro-pyrimidinonesnes, homologues of SR 47436, was identified as AT1 receptor antagonists. The best compounds showed high affinity for the AT1 receptor (rat liver membrane preparation) with IC%'s in the nanomolar range. Active p.o. in rats in an AII infused model, they ate inacdve in cynomolgus monkeys.

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