Design and Synthesis of Pyrido[1,2-e]purin-4(3H)-one Derivatives as Potential PDE 5 Inhibitors

作     者：Guang Xin XIA Jian Feng LI Shun An LAI Ai Ming PENG Shu Jun ZHANG Xiao Hui WEI Xin Jian CHEN Jing Shan SHEN Ru Yun JI 

作者机构：Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 Topharman Shanghai Co. Ltd Shanghai 201209 Graduate School of the Chinese Academy of Sciences Beijing 100039 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2005年第16卷第10期

页      码：1283-1286页

摘      要：A novel series of pyrido[ 1,2-e]purin-4（3H）-one derivatives containing polar substituents on 5＇-position were designed and prepared as potential PDE5 inhibitors. This paper reports the synthetic routes, 1H-NMR data, and the PDE5 inhibitory activities of the target compounds. The polar piperazinyl group contained （on 5＇-position） compound, 3B2, showed the highest activity among the tested derivatives but less potency than sildenafil 1.

主 题 词：Pyrido[1,2-e]purin-4(3H)-one PDE5 inhibitor sildenafil erectile dysfunction (ED). 

学科分类：081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 070303[070303] 0703[理学-化学类] 

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