Literature DB >> 23122821

Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors.

Yutaka Mori1, Yasuyuki Ogawa, Akiyoshi Mochizuki, Yuji Nakamura, Chie Sugita, Shojiro Miyazaki, Kazuhiko Tamaki, Yumi Matsui, Mizuki Takahashi, Takahiro Nagayama, Yoko Nagai, Shin-ichi Inoue, Takahide Nishi.   

Abstract

Utilizing X-ray crystal structure analysis, (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides were designed and identified as renin inhibitors. The most potent compound 15 demonstrated favorable pharmacokinetic and pharmacodynamic profiles in rat.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 23122821     DOI： 10.1016/j.bmcl.2012.09.103

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


  3 in total

1.  Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.

Authors:  Takeru Ehara; Osamu Irie; Takatoshi Kosaka; Takanori Kanazawa; Werner Breitenstein; Philipp Grosche; Nils Ostermann; Masaki Suzuki; Shimpei Kawakami; Kazuhide Konishi; Yuko Hitomi; Atsushi Toyao; Hiroki Gunji; Frederic Cumin; Nikolaus Schiering; Trixie Wagner; Dean F Rigel; Randy L Webb; Jürgen Maibaum; Fumiaki Yokokawa
Journal:  ACS Med Chem Lett       Date:  2014-04-21       Impact factor: 4.345

2.  Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.

Authors:  Yasuhiro Imaeda; Hidekazu Tokuhara; Yoshiyuki Fukase; Ray Kanagawa; Yumiko Kajimoto; Keiji Kusumoto; Mitsuyo Kondo; Gyorgy Snell; Craig A Behnke; Takanobu Kuroita
Journal:  ACS Med Chem Lett       Date:  2016-09-12       Impact factor: 4.345

Review 3.  Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules.

Authors:  Krishnappa Ramya; Ramalingam Suresh; Honnavalli Yogish Kumar; B R Prashantha Kumar; N B Sridhara Murthy
Journal:  Bioorg Med Chem       Date:  2020-03-28       Impact factor: 3.641
  3 in total

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