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

查看全文 作  者:Guang Xin [1,3]XIA;Jian Feng [1,3]LI;Shun An [2]LAI;Ai Ming [2]PENG;Shu Jun [1]ZHANG;Xiao Hui [1]WEI;Xin Jian [1]CHEN;Jing Shan [1]SHEN;Ru Yun [1]JI 高影响力作者 机构地区:[1]Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203;[2]Topharman Shanghai Co., Ltd, Shanghai 201209;[3]Graduate School of the Chinese Academy of Sciences, Beijing 100039高影响力机构 出  处:《Chinese Chemical Letters》索引2005年第16卷第10期,共4页高影响力期刊 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. 关 键 词:嘌呤 衍生物 抑制剂 磷酸二酯酶 合成方法
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