alpha(v)beta(3) antagonists based on a central thiophene scaffold

Authors
Peyman, A Scheunemann, KH Will, DW Knolle, J Wehner, V Breipohl, G Stilz, HU Carniato, D Ruxer, JM Gourvest, JF Auberval, M Doucet, B Baron, R Gaillard, M Gadek, TR Bodary, S
Citation
A. Peyman et al., alpha(v)beta(3) antagonists based on a central thiophene scaffold, BIOORG MED, 11(15), 2001, pp. 2011-2015
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
15
Year of publication
2001
Pages
2011 - 2015
Database
ISI
SICI code
0960-894X(20010806)11:15<2011:AABOAC>2.0.ZU;2-2
Abstract
A series of novel, highly potent alpha (v)beta (3) antagonists based on a t hiophene scaffold and containing an acylguanidine as an Arg-mimetic is desc ribed. A number of structural features, such as cyclic versus open guanidin e and a variety of lipophilic side chains, carbamates, sulfonamides and bet a -amino acids were explored with respect to inhibition of alpha (v)beta (3 ) mediated cell adhesion and selectivity versus alpha (IIb)beta (3) binding . In addition, compound 19 was found to be active in the TPTX model of oste oporosis. (C) 2001 Published by Elsevier Science Ltd.