Design and synthesis of novel imidazo[1,2-a]quinoxalines as PDE4 inhibitors

被引:31
作者
Deleuze-Masquéfa, C
Gerebtzoff, G
Subra, G
Fabreguettes, JR
Ovens, A
Carraz, M
Strub, MP
Bompart, J
George, P
Bonnet, PA
机构
[1] Fac Pharm Montpellier, Lab Chim Organ Pharmaceut, F-34093 Montpellier 5, France
[2] Fac Pharm Montpellier, Ctr Biochim Struct, F-34093 Montpellier 5, France
[3] Sanofi Synthelabo Rech, Dept Rech Syst Nerveux Cent, F-92220 Bagneux, France
关键词
phosphodiesterase; 4; imidazo[1,2-a]quinoxaline; phosphodiesterase inhibition;
D O I
10.1016/j.bmc.2003.11.034
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
New imidazo[1,2-a]quinoxaline derivatives have been synthesised by condensation of an appropriate alpha-aminoalcohol with a quinoxaline followed by intramolecular cyclisation and nucleophilic substitutions. Their phosphodiesterase inhibitory activities have been assessed on a preparation of the PDE4 isoform purified from a human alveolar epithelial cell line (A549). These studies showed potent inhibitory properties that emphasize the importance of a methyl amino group at position 4 and a weakly hindered group at position 1. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1129 / 1139
页数:11
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