Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives

Guangxin Xia; Jianfeng Li; Aiming Peng; Shunan Lai; Shujun Zhang; Jingshan Shen; Zhonghua Liu; Xinjian Chen; Ruyun Ji

doi:10.1016/j.bmcl.2005.03.102

Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2790-4. doi: 10.1016/j.bmcl.2005.03.102.

Authors

Guangxin Xia¹, Jianfeng Li, Aiming Peng, Shunan Lai, Shujun Zhang, Jingshan Shen, Zhonghua Liu, Xinjian Chen, Ruyun Ji

Affiliation

¹ Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Zhangjiang High-Tech Park, Shanghai.

PMID: 15878277
DOI: 10.1016/j.bmcl.2005.03.102

Abstract

Synthesis and primary SAR of a novel series of 2-phenylpyrido[1,2-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.

MeSH terms

3',5'-Cyclic-GMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 5
Phosphodiesterase Inhibitors / chemical synthesis*
Phosphodiesterase Inhibitors / chemistry
Phosphodiesterase Inhibitors / pharmacology*
Phosphoric Diester Hydrolases / drug effects*
Purines / chemical synthesis*
Purines / chemistry
Purines / pharmacology*
Structure-Activity Relationship

Substances

Phosphodiesterase Inhibitors
Purines
Phosphoric Diester Hydrolases
3',5'-Cyclic-GMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 5