title: Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.
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.
authors.affiliation: Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Zhangjiang High-Tech Park, Shanghai.
authors.forename: Guangxin
authors.initials: G
authors.lastname: Xia
authors.forename: Jianfeng
authors.initials: J
authors.lastname: Li
authors.forename: Aiming
authors.initials: A
authors.lastname: Peng
authors.forename: Shunan
authors.initials: S
authors.lastname: Lai
authors.forename: Shujun
authors.initials: S
authors.lastname: Zhang
authors.forename: Jingshan
authors.initials: J
authors.lastname: Shen
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Liu
authors.forename: Xinjian
authors.initials: X
authors.lastname: Chen
authors.forename: Ruyun
authors.initials: R
authors.lastname: Ji
mesh_terms: D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000187:drug effects*; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010726:Phosphodiesterase Inhibitors; D011687:Purines; D010727:Phosphoric Diester Hydrolases; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5