NONPEPTIDIC INHIBITORS OF NEUTRAL ENDOPEPTIDASE-24.11 .1. DISCOVERY AND OPTIMIZATION OF POTENCY

Authors
DELOMBAERT S BLANCHARD L TAN J SAKANE Y BERRY C GHAI RD
Citation
S. Delombaert et al., NONPEPTIDIC INHIBITORS OF NEUTRAL ENDOPEPTIDASE-24.11 .1. DISCOVERY AND OPTIMIZATION OF POTENCY, Bioorganic & medicinal chemistry letters, 5(2), 1995, pp. 145-150
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
2
Year of publication
1995
Pages
145 - 150
Database
ISI
SICI code
0960-894X(1995)5:2<145:NIONE.>2.0.ZU;2-M
Abstract
Although based on a single alpha-amino acid residue, N-phosphonomethyl -(S)-(4-phenyl)phenylalanine (2) was discovered to produce strong inhi bition of the zinc metalloprotease, neutral endopeptidase (NEP 24.11). Structural optimization of this new lead culminated with the design o f the phosphonic acid tetrazole 17 (CGS 26303), a non-peptidic and ext remely potent NEP inhibitor.