NONPEPTIDIC INHIBITORS OP NEUTRAL ENDOPEPTIDASE-24.11 .2. DESIGN AND PHARMACOLOGY OF ORALLY-ACTIVE PHOSPHONATE PRODRUGS

Authors
DELOMBAERT S BLANCHARD L BERRY C GHAI RD TRAPANI AJ
Citation
S. Delombaert et al., NONPEPTIDIC INHIBITORS OP NEUTRAL ENDOPEPTIDASE-24.11 .2. DESIGN AND PHARMACOLOGY OF ORALLY-ACTIVE PHOSPHONATE PRODRUGS, Bioorganic & medicinal chemistry letters, 5(2), 1995, pp. 151-154
Citations number
8
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
151 - 154
Database
ISI
SICI code
0960-894X(1995)5:2<151:NIONE.>2.0.ZU;2-N
Abstract
Prodrugs of 1 (CGS 26303), a novel non-peptidic neutral endopeptidase (NEP 24.11) inhibitor, have been designed. In particular, the diphenyl phosphonate 6 (CGS 26393) was found to be a potent, orally bioavailabl e and long-acting NEP inhibitor. Accordingly, 6 protected atrial natri uretic peptide from enzymatic degradation and displayed a significant antihypertensive activity in the DOCA-salt rat.