Literature DB >> 11549447

The discovery of novel, potent and selective PDE5 inhibitors.

Y Bi1, P Stoy, L Adam, B He, J Krupinski, D Normandin, R Pongrac, L Seliger, A Watson, J E Macor.   

Abstract

The design and synthesis of a novel scaffold for potent and selective PDE5 inhibitors are described. Compound 3a was more potent (PDE5 IC50=0.31 nM) and selective (>10,000-fold vs PDE1 and 160-fold selective vs PDE6) PDE5 inhibitor than sildenafil.

Entities:  

Mesh：

Substances：

Year:  2001        PMID： 11549447     DOI： 10.1016/s0960-894x(01)00466-8

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


  3 in total

1.  Sildenafil triggers tumor lethality through altered expression of HSP90 and degradation of PKD2.

Authors:  Lu Chen; Yang Liu; Alexander Becher; Kristina Diepold; Evi Schmid; Adrian Fehn; Cornelia Brunner; Arefeh Rouhi; Gabriela Chiosis; Marcus Cronauer; Thomas Seufferlein; Ninel Azoitei
Journal:  Carcinogenesis       Date:  2020-10-15       Impact factor: 4.944

2.  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

3.  Multi-component one-pot synthesis and antimicrobial activities of 3-methyl-1,4-diphenyl-7-thioxo-4,6,8,9-tetrahydro-pyrazolo[5,4-b]pyrimidino[5,4-e]pyridine-5-one and related derivatives.

Authors:  Talaat I El-Emary; Shawkat A Abd El-Mohsen
Journal:  Molecules       Date:  2012-12-06       Impact factor: 4.411
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.