1-苄基黄嘌呤对环磷酸腺苷磷酸二酯酶4同工酶的影响。

Effects of 1-benzylxanthines on cyclic AMP phosphodiesterase 4 isoenzyme.

作者信息

Suzuki Hirokazu, Sawanishi Hiroyuki, Nomura Masaaki, Shimada Tsutomu, Miyamoto Ken-Ichi

机构信息

Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.

出版信息

Biol Pharm Bull. 2006 Jan;29(1):131-4. doi: 10.1248/bpb.29.131.

DOI:10.1248/bpb.29.131

PMID:16394525

Abstract

Based on our results regarding the structure-activity relationships of alkylxanthines and imidazo[2,1-i]purines as phosphodiesterase 4 (PDE4) inhibitors, we designed new 1-benzylxanthines and investigated their PDE4 inhibitory activities. 3,7-Dihydro-7-acetonyl-1-(2,4-dichlorobenzyl)-3-propyl-1H-purine-2,4-dione (2h) exhibited both more selective and more potent PDE4 inhibitory activity than rolipram and XT-611.

摘要

基于我们关于烷基黄嘌呤和咪唑并[2,1-i]嘌呤作为磷酸二酯酶4（PDE4）抑制剂的构效关系的研究结果，我们设计了新型1-苄基黄嘌呤并研究了它们的PDE4抑制活性。3,7-二氢-7-丙酮基-1-(2,4-二氯苄基)-3-丙基-1H-嘌呤-2,4-二酮（2h）表现出比咯利普兰和XT-611更具选择性和更强的PDE4抑制活性。