Literature DB >> 25455484

The discovery of avanafil for the treatment of erectile dysfunction: a novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor.

Toshiaki Sakamoto1, Yuichi Koga1, Masataka Hikota1, Kenji Matsuki1, Michino Murakami2, Kohei Kikkawa2, Kotomi Fujishige3, Jun Kotera3, Kenji Omori4, Hiroshi Morimoto5, Koichiro Yamada1.   

Abstract

Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and highly selective phosphodiesterase 5 inhibitors. Among them, we successfully found 10j (avanafil) which exhibited a potent relaxant effect on isolated rabbit cavernosum (EC30=2.1 nM) and a high isozyme selectivity.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Avanafil; Erectile dysfunction; PDE5; PDE6

Mesh：

Substances：

Year:  2014        PMID： 25455484     DOI： 10.1016/j.bmcl.2014.10.008

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


  4 in total

1.  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

2.  Avanafil Inhibits the Contractility of the Isolated Caprine Detrusor Muscle.

Authors:  Aakash Dhruva; Venkata Kuppuswamy Hamsavardhini; Shiny Kamatham; Anushka Kataria; Aniket Kumar; Margaret Shanthi; Jacob Peedicayil
Journal:  Int J Appl Basic Med Res       Date:  2019-10-11

3.  Identification, synthesis and characterization of avanafil process impurities and determination by UPLC.

Authors:  Mengmeng Zhao; Xiaoxia Wu; Zengda Yu; Yunkai Sun; Zhao Liu; Jinqiao Yuan; Hu Liu; Yiping Jin
Journal:  RSC Adv       Date:  2022-03-24       Impact factor: 3.361

4.  Papaverine hydrochloride containing nanostructured lyotropic liquid crystal formulation as a potential drug delivery system for the treatment of erectile dysfunction.

Authors:  Szilvia Berkó; Stella Zsikó; Gábor Deák; Attila Gácsi; Anita Kovács; Mária Budai-Szűcs; László Pajor; Zoltán Bajory; Erzsébet Csányi
Journal:  Drug Des Devel Ther       Date:  2018-09-12       Impact factor: 4.162
  4 in total

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