Combined NK1 and N-2 tachykinin receptor antagonists: Synthesis and structure-activity relationships of novel oxazolidine analogues

Authors
Nishi, T Fukazawa, T Ishibashi, K Nakajima, K Sugioka, Y Iio, Y Kurata, H Itoh, K Mukaiyama, O Satoh, Y Yamaguchi, T
Citation
T. Nishi et al., Combined NK1 and N-2 tachykinin receptor antagonists: Synthesis and structure-activity relationships of novel oxazolidine analogues, BIOORG MED, 9(6), 1999, pp. 875-880
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
6
Year of publication
1999
Pages
875 - 880
Database
ISI
SICI code
0960-894X(19990322)9:6<875:CNANTR>2.0.ZU;2-5
Abstract
We report herein the synthesis and structure-activity relationships of a se ries of novel oxazolidine analogues with regards to NK1 and NK2 tachykinin receptor binding affinity. Among this series of oxazolidine analogues, some compounds exhibited excellent high binding affinities for both NK1 and NK2 receptors. In addition, we describe the inhibitory effect in vivo on SP-in duced airway vascular hyperpermeability and NKA-induced bronchoconstriction in guinea pigs. (C) 1999 Elsevier Science Ltd. All rights reserved.