Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives |
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| Authors: | Xia Guangxin Li Jianfeng Peng Aiming Lai Shunan Zhang Shujun Shen Jingshan Liu Zhonghua Chen Xinjian Ji Ruyun |
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| Institution: | Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Zhangjiang High-Tech Park, Shanghai. |
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| Abstract: | Synthesis and primary SAR of a novel series of 2-phenylpyrido1,2-e]purin-4(3H)-one derivatives with piperazinyl sulfonamide substituents were described herein. As potential PDE5 inhibitors for erectile dysfunction (ED) treatment, representative compounds exhibit improved selectivity versus PDE1 and PDE6. Meanwhile, compound 3e demonstrated functional efficacy on rabbit corpus cavernosum strip in vitro. |
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