Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase

Authors
Moormann, AE Metz, S Toth, MV Moore, WM Jerome, G Kornmeier, C Manning, P Hansen, DW Pitzele, BS Webber, RK
Citation
Ae. Moormann et al., Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase, BIOORG MED, 11(19), 2001, pp. 2651-2653
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
19
Year of publication
2001
Pages
2651 - 2653
Database
ISI
SICI code
0960-894X(20011008)11:19<2651:SHAIOH>2.0.ZU;2-E
Abstract
The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepine s were examined as inhibitors or the three human NOS isoforms. The effect o r ring substitution of the 5-carbon for a heteroatom is presented. Potencie s (IC50's) for these inhibitors are in the low micromolar range for hi-NOS with some examples exhibiting a 500x selectivity versus hec-NOS. (C) 2001 E lsevier Science Ltd. All rights reserved.