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

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

下载PDF

导出

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. 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.

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

机构地区 Shanghai Institute of Materia Medica Topharman Shanghai Co. Graduate School of the Chinese Academy of Sciences

出处《Chinese Chemical Letters》 SCIE CAS CSCD 2005年第10期1283-1286,共4页 中国化学快报（英文版）

关键词 Pyrido[1 2-e]purin-4（3H）-one PDE5 inhibitor SILDENAFIL erectile dysfunction （ED）. Pyrido[1,2-e]purin-4（3H）-one, PDE5 inhibitor, sildenafil, erectile dysfunction （ED）.

分类号 O626 [理学—有机化学] O623.624 [理学—有机化学]

引文网络
相关文献

参考文献13

1D.P. Rotella, Nat. Rev. Drug Discov., 2002, 1,674.
2S.H. Francis, I. V. Turko, J. D. Corbin, Prog. Nucleic Acid Res. Mol. Biol., 2000, 65, 1.
3J.C. Lanter, Z. Sui, M. J. Macielag, et al., J Med. Chem., 2004, 47, 656.
4J.A. Beavo, Physiol Rev., 1995, 75, 725.
5D.A. Fox, M. L. Campbell, Y. S. Blocker, Neurotoxicology, 1997, 18, 645.
6D.P. Rotella, Z. Sun, Y. Zhu, et al., J. Med. Chem., 2000, 43, 1257.
7N.K. Terrett, A. S. Bell, D. Brown, et al., Bioorg. Med. Chem. Lett., 1996, 6, 1819.
8H. Haning, U. Niewohner, T. Schenke, et al., Bioorg. Med. Chem. Lett., 2002, 12, 865.
9J.C. Teulade, R. Escale, J. C. Rossi, et al., Aust. J. Chem., 1982, 35, 1761.
10F. Pinguet, S. Mavel, C. Galtier, et al, Pharmazie, 1999, 54, 876.