alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: Carbonyl group modification and alpha-substitution

Authors
Boger, DL Miyauchi, H Hedrick, MP
Citation
Dl. Boger et al., alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: Carbonyl group modification and alpha-substitution, BIOORG MED, 11(12), 2001, pp. 1517-1520
Citations number
28
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
12
Year of publication
2001
Pages
1517 - 1520
Database
ISI
SICI code
0960-894X(20010618)11:12<1517:AHIOFA>2.0.ZU;2-C
Abstract
Two sets of novel analogues of the recently disclosed alpha -keto heterocyc le inhibitors of fatty acid amide hydrolase (FAAH), the enzyme responsible for regulation of endogenous oleamide and anandamide, were synthesized and evaluated in order to clarify a role of the electrophilic carbonyl group an d structural features important for their activity. Both the electrophilic carbonyl and the degree of alpha -substitution markedly affect inhibitor po tency. (C) 2001 Elsevier Science Ltd. All rights reserved.