Literature DB >> 15878277

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

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

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.

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Year:  2005        PMID: 15878277     DOI: 10.1016/j.bmcl.2005.03.102

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Emerging approaches for the syntheses of bicyclic imidazo[1,2-x]-heterocycles.

Authors:  Christopher Hulme; Yeon-Sun Lee
Journal:  Mol Divers       Date:  2008-04-12       Impact factor: 2.943

2.  Discovery of potent inhibitors for phosphodiesterase 5 by virtual screening and pharmacophore analysis.

Authors:  Chien-yu Chen; Yea-huey Chang; Da-tian Bau; Hung-jin Huang; Fuu-jen Tsai; Chang-hai Tsai; Calvin Yu-chian Chen
Journal:  Acta Pharmacol Sin       Date:  2009-07-13       Impact factor: 6.150

3.  Ethyl 5-methyl-imidazo[1,2-a]pyridine-2-carboxyl-ate.

Authors:  Jin-Hua Yao; Lan-Fang Wang; Bing Guo; Kang An; Jian-Ning Guan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-07-14

4.  Pharmacophore elucidation and molecular docking studies on phosphodiesterase-5 inhibitors.

Authors:  Awwad Abdoh Radwan
Journal:  Bioinformation       Date:  2015-02-28

5.  Investigation of PDE5/PDE6 and PDE5/PDE11 selective potent tadalafil-like PDE5 inhibitors using combination of molecular modeling approaches, molecular fingerprint-based virtual screening protocols and structure-based pharmacophore development.

Authors:  Gülru Kayık; Nurcan Ş Tüzün; Serdar Durdagi
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

6.  Synthesis and Spectroscopic Analysis of Novel 1H-Benzo[d]imidazoles Phenyl Sulfonylpiperazines.

Authors:  Amjad M Qandil
Journal:  Pharmaceuticals (Basel)       Date:  2012-05-03
  6 in total

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