Benzofuran based PDE4 inhibitors

被引:15
作者
McGarry, DG
Regan, JR
Volz, FA
Hulme, C
Moriarty, KJ
Djuric, SW
Souness, JE
Miller, BE
Travis, JJ
Sweeney, DM
机构
[1] Rhone Poulenc Rorer, Dept Med Chem, Collegeville, PA 19426 USA
[2] Rhone Poulenc Rorer, Dept Inflammat Biol, Collegeville, PA 19426 USA
[3] Rhone Poulenc Rorer, Dept Inflammat Biol, Dagenham RM10 7XS, Essex, England
关键词
D O I
10.1016/S0968-0896(99)00038-3
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Replacement of the 3,4-dialkoxyphenyl substructure common to a number of PDE4 inhibitors with a 2-alkyl-7-methoxybenzofuran unit is described. This substitution can result in either enhancement or substantial reductions in PDE4 inhibitory activity depending on the system to which it is applied. An in 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.
引用
收藏
页码:1131 / 1139
页数:9
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