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

TQ452; 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 pip...

Full description

Saved in:
Bibliographic Details
Published in中国化学快报（英文版） Vol. 16; no. 10; pp. 1283 - 1286
Main Authors 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
Format Journal Article
LanguageEnglish
Published Graduate School of the Chinese Academy of Sciences, Beijing 100039%Topharman Shanghai Co., Ltd, Shanghai 201209%Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences,Chinese Academy of Sciences, Shanghai 201203 01.10.2005
Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences,Chinese Academy of Sciences, Shanghai 201203
Subjects
Pyrido[1,2-e]purin-4(3H)-one,PDE5 inhibitor,sildenafil,erectile dysfunction (ED)
Online AccessGet full text

Cover

More Information
Summary:TQ452; 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.
ISSN:1001-8417
1878-5964