Literature DB >> 28359792

4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures.

Masaki Meguro1, Satoru Miyauchi2, Yukiko Kanao2, Satoru Naito2, Kanae Suzuki2, Shinichi Inoue2, Keisuke Yamada2, Tsuyoshi Homma2, Kiyoshi Chiba2, Futoshi Nara2, Shinji Furuzono2.   

Abstract

2,2,2-Trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-yl}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol 1 was identified as a novel potent aldosterone synthase inhibitor. Despite large species differences, compound 1 inhibits both human and rodent CYP11B2 in a nano-molar range.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Aldosterone; Aldosterone synthase inhibitor; Amino-pyrimidine; CYP11B1; CYP11B2

Mesh:

Substances:

Year:  2017        PMID: 28359792     DOI: 10.1016/j.bmcl.2017.03.034

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


  2 in total

Review 1.  Human cytochrome P450 enzymes 5-51 as targets of drugs and natural and environmental compounds: mechanisms, induction, and inhibition - toxic effects and benefits.

Authors:  Slobodan P Rendic; F Peter Guengerich
Journal:  Drug Metab Rev       Date:  2018-08       Impact factor: 4.518

2.  N-Aryl-7-hydroxy-5-oxo-2,3-dihydro-1H,5H-pyrido-[3,2,1-ij]quinoline-6-carboxamides. The Synthesis and Effects on Urinary Output.

Authors:  Igor V Ukrainets; Lyudmila V Sidorenko; Mykola Y Golik; Igor M Chernenok; Lina A Grinevich; Alexandra A Davidenko
Journal:  Sci Pharm       Date:  2018-04-09
  2 in total

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