| Design and Synthesis of Pyrido[1,2-e]purin-4（3H）-one Derivatives as Potential PDE 5 Inhibitors |
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| 引用本文： | 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. Design and Synthesis of Pyrido[1,2-e]purin-4（3H）-one Derivatives as Potential PDE 5 Inhibitors[J]. 中国化学快报, 2005, 16(10): 1283-1286 |
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| 作者姓名： | 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 |
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| 作者单位： | [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 |
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| 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.
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| 关 键 词： | 嘌呤 衍生物 抑制剂 磷酸二酯酶 合成方法 |
| 收稿时间： | 2004-12-20 |
Design and Synthesis of Pyrido[1,2-e]purin-4(3H)-one Derivatives as Potential PDE 5 Inhibitors |
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| 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. Design and Synthesis of Pyrido[1,2-e]purin-4(3H)-one Derivatives as Potential PDE 5 Inhibitors[J]. Chinese Chemical Letters, 2005, 16(10): 1283-1286 |
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| 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 |
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| Abstract: | 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. |
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| Keywords: | Pyrido[1 2-e]purin-4(3H)-one PDE5 inhibitor sildenafil erectile dysfunction (ED). |
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