DUAL METALLOPROTEASE INHIBITORS .3. UTILIZATION OF BICYCLIC AND MONOCYCLIC DIAZEPINONE BASED MERCAPTOACETYLS

Authors
ROBL JA SUN CQ SIMPKINS LM RYONO DE BARRISH JC KARANEWSKY DS ASAAD MM SCHAEFFER TR TRIPPODO NC
Citation
Ja. Robl et al., DUAL METALLOPROTEASE INHIBITORS .3. UTILIZATION OF BICYCLIC AND MONOCYCLIC DIAZEPINONE BASED MERCAPTOACETYLS, Bioorganic & medicinal chemistry letters, 4(16), 1994, pp. 2055-2060
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
16
Year of publication
1994
Pages
2055 - 2060
Database
ISI
SICI code
0960-894X(1994)4:16<2055:DMI.UO>2.0.ZU;2-J
Abstract
A series of bicyclic and monocyclic diazepinones were incorporated as conformationally restricted dipeptide surrogates in mercaptoacetyl dip eptide dual-acting ACE/NEP inhibitors. A comparison was made between t hese two classes of compounds as well as with the previously disclosed ACE/NEP inhibitor 1. Compound 2a was found to exhibit high potency ve rsus both enzymes in vitro as well as in vivo.