Benzofuran based PDE4 inhibitors

Authors
McGarry, DG Regan, JR Volz, FA Hulme, C Moriarty, KJ Djuric, SW Souness, JE Miller, BE Travis, JJ Sweeney, DM
Citation
Dg. Mcgarry et al., Benzofuran based PDE4 inhibitors, BIO MED CH, 7(6), 1999, pp. 1131-1139
Citations number
32
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
6
Year of publication
1999
Pages
1131 - 1139
Database
ISI
SICI code
0968-0896(199906)7:6<1131:BBPI>2.0.ZU;2-1
Abstract
Replacement of the 3,4-dialkoxyphenyl substructure common to a number of PD E4 inhibitors with a 2-alkyl-7-methoxybenzofuran unit is described. This su bstitution can result in either enhancement or substantial reductions in PD E4 inhibitory activity depending on the system to which it is applied. An i n vitro SAR study of a potent series of 4-(2-heteroaryl-ethyl)-benzofurans 26 is also presented. (C) 1999 Elsevier Science Ltd. All rights reserved.