N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: An orally active neurokinin NK1/NK2 antagonist

Citation
M. Gerspacher et al., N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: An orally active neurokinin NK1/NK2 antagonist, BIOORG MED, 10(13), 2000, pp. 1467-1470
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
13
Year of publication
2000
Pages
1467 - 1470
Database
ISI
SICI code
0960-894X(20000703)10:13<1467:N>2.0.ZU;2-P
Abstract
The stereoselective synthesis of N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo- azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide (4) and its NK1 and NK2 receptor binding properties are reported. In addition the potent inhibitory effects in vivo on sar(9)-SP- and -beta-Ala-NKA-induc ed airway bronchoconstriction in guinea pigs are demonstrated. (C) 2000 Els evier Science Ltd. All rights reserved.