VALSARTAN, A POTENT, ORALLY-ACTIVE ANGIOTENSIN-II ANTAGONIST DEVELOPED FROM THE STRUCTURALLY NEW AMINO-ACID SERIES

Authors
BUHLMAYER P FURET P CRISCIONE L DEGASPARO M WHITEBREAD S SCHMIDLIN T LATTMANN R WOOD J
Citation
P. Buhlmayer et al., VALSARTAN, A POTENT, ORALLY-ACTIVE ANGIOTENSIN-II ANTAGONIST DEVELOPED FROM THE STRUCTURALLY NEW AMINO-ACID SERIES, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 29-34
Citations number
17
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
29 - 34
Database
ISI
SICI code
0960-894X(1994)4:1<29:VAPOAA>2.0.ZU;2-6
Abstract
Starting from the structure of DuP-753 and a 3-dimensional model of th e pentapeptide Tyr-Ile-His-Pro-Ile, a series of new and highly potent antagonists has been designed where the imidazole moiety of the Du Pon t compound has been-replaced by an N-acylated aminoacid residue. VALSA RTAN (Ex. 4e, CGP48933, -(1H-tetrazol-5-yl-)biphenyl-4-yl]methyl}-vali ne), has been selected for clinical investigation.