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Quinazolinones 2: QSAR and in vivo characterization of AT1 selective AII antagonists

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
3
Issue
6
Identifiers
DOI: 10.1016/s0960-894x(00)80335-2

Abstract

Abstract The structure activity relatoionship, linear regression analysis and in vivo evaluation of a series of substituted 2-butyl-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]quinazolin-4(1H)-ones as antagonists of the AT 1 receptor for angiotensin II is presented. L-159,093 (2-butyl-6-(N-isopropyl-N-methyl-carbamoyl)amino-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]quin azolin-4(1H)-one (IC 50=0.1nM rabbit aorta) is shown to be a potent orally active AII antagonist in rats and rhesus.

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