Literature DB >> 15686947

Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.

Wu Yang1, Yufeng Wang, Jacques Y Roberge, Zhengping Ma, Yalei Liu, R Michael Lawrence, David P Rotella, Ramakrishna Seethala, Jean H M Feyen, John K Dickson.   

Abstract

A structure-activity relationship study of the amine portion of the calcilytic compound NPS-2143 resulted in the discovery of substituted 2-benzylpyrrolidines as replacements for the 1,1-dimethyl-2-naphthalen-2-yl-ethylamine. When compared to NPS-2143, a newly discovered compound, 3h, exhibited similar potency as a calcium-sensing receptor (CaR) antagonist and a superior human ether-a-go-go related gene (hERG) profile.

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Year:  2005        PMID： 15686947     DOI： 10.1016/j.bmcl.2004.11.071

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


  11 in total

1.  Copper(II)-catalyzed enantioselective intramolecular carboamination of alkenes.

Authors:  Wei Zeng; Sherry R Chemler
Journal:  J Am Chem Soc       Date:  2007-10-05       Impact factor: 15.419

2.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

3.  Stereoselective and Regioselective Synthesis of Heterocycles via Copper-Catalyzed Additions of Amine Derivatives and Alcohols to Alkenes.

Authors:  Sherry R Chemler; Shuklendu D Karyakarte; Zainab M Khoder
Journal:  J Org Chem       Date:  2017-09-29       Impact factor: 4.354

4.  Evolution of copper(II) as a new alkene amination promoter and catalyst.

Authors:  Sherry R Chemler
Journal:  J Organomet Chem       Date:  2011-01-01       Impact factor: 2.369

5.  Melamine induces Ca2+-sensing receptor activation and elicits apoptosis in proximal tubular cells.

Authors:  Allen J Yiu; Cliff-Lawrence Ibeh; Sanjit K Roy; Bidhan C Bandyopadhyay
Journal:  Am J Physiol Cell Physiol       Date:  2017-04-05       Impact factor: 4.249

6.  Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity.

Authors:  Dianqing Sun; Michael S Scherman; Victoria Jones; Julian G Hurdle; Lisa K Woolhiser; Susan E Knudson; Anne J Lenaerts; Richard A Slayden; Michael R McNeil; Richard E Lee
Journal:  Bioorg Med Chem       Date:  2009-04-09       Impact factor: 3.641

7.  Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine.

Authors:  Xiaoying Zhang; Tao Jin; Na Shi; Linbo Yao; Xinmin Yang; Chenxia Han; Li Wen; Dan Du; Peter Szatmary; Rajarshi Mukherjee; Tingting Liu; Qing Xia; David N Criddle; Wei Huang; Michael Chvanov; Robert Sutton
Journal:  Front Physiol       Date:  2019-01-15       Impact factor: 4.566

Review 8.  Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review.

Authors:  Wan-Yin Fang; L Ravindar; K P Rakesh; H M Manukumar; C S Shantharam; Njud S Alharbi; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2019-04-10       Impact factor: 6.514

9.  Allosteric modulation of the calcium-sensing receptor.

Authors:  Anders A Jensen; Hans Bräuner-Osborne
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363

Review 10.  Structure and function of the human calcium-sensing receptor: insights from natural and engineered mutations and allosteric modulators.

Authors:  Jianxin Hu; Allen M Spiegel
Journal:  J Cell Mol Med       Date:  2007 Sep-Oct       Impact factor: 5.310
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