NEW ANALOGS OF N-(2-AMINOETHYL)-4-CHLOROBENZAMIDE (RO 16-6491) - SOMEOF THE MOST POTENT MONOAMINE OXIDASE-B INACTIVATORS

Authors
ANNAN N SILVERMAN RB
Citation
N. Annan et Rb. Silverman, NEW ANALOGS OF N-(2-AMINOETHYL)-4-CHLOROBENZAMIDE (RO 16-6491) - SOMEOF THE MOST POTENT MONOAMINE OXIDASE-B INACTIVATORS, Journal of medicinal chemistry, 36(24), 1993, pp. 3968-3970
Citations number
11
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
36
Issue
24
Year of publication
1993
Pages
3968 - 3970
Database
ISI
SICI code
0022-2623(1993)36:24<3968:NAON(1>2.0.ZU;2-Q
Abstract
A series of halo- and nitro-substituted analogues of N-(2-aminoethyl)b enzamide has been synthesized. All of the compounds are competitive, t ime-dependent inhibitors of monoamine oxidase-B (MAO-B), but upon dial ysis complete return of enzyme activity is observed for all compounds. Therefore, these are mechanism-based reversible inhibitors of MAO-B. The relative potencies of the compounds are rationalized in terms of s teric and hydrophobic effects.