Literature DB >> 20685119

Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).

Marc Gerspacher1, Eva Altmann, René Beerli, Thomas Buhl, Ralf Endres, Rainer Gamse, Jacques Kameni-Tcheudji, Michaela Kneissel, Karl Heinz Krawinkler, Martin Missbach, Alfred Schmidt, Klaus Seuwen, Sven Weiler, Leo Widler.   

Abstract

A series of novel benzimidazole derivatives has been designed via a scaffold morphing approach based on known calcilytics chemotypes. Subsequent lead optimisation led to the discovery of penta-substituted benzimidazoles that exhibit attractive in vitro and in vivo calcium-sensing receptor (CaSR) inhibitory profiles. In addition, synthesis and structure-activity relationship data are provided. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20685119     DOI: 10.1016/j.bmcl.2010.07.016

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


  2 in total

Review 1.  International Union of Basic and Clinical Pharmacology. CVIII. Calcium-Sensing Receptor Nomenclature, Pharmacology, and Function.

Authors:  Katie Leach; Fadil M Hannan; Tracy M Josephs; Andrew N Keller; Thor C Møller; Donald T Ward; Enikö Kallay; Rebecca S Mason; Rajesh V Thakker; Daniela Riccardi; Arthur D Conigrave; Hans Bräuner-Osborne
Journal:  Pharmacol Rev       Date:  2020-07       Impact factor: 25.468

2.  Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone.

Authors:  Yuko Shinagawa; Teruhiko Inoue; Takeo Katsushima; Toshihiro Kiguchi; Taku Ikenogami; Naoki Ogawa; Kenji Fukuda; Kazuyuki Hirata; Kazuhito Harada; Masaki Takagi; Takashi Nakagawa; Shuichi Kimura; Yushi Matsuo; Mariko Maekawa; Mikio Hayashi; Yuki Soejima; Mitsuru Takahashi; Masanori Shindo; Hiromasa Hashimoto
Journal:  ACS Med Chem Lett       Date:  2010-12-29       Impact factor: 4.345

  2 in total

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