Literature DB >> 16216508

Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.

Ashvinikumar V Gavai1, Roy J Vaz, Amarendra B Mikkilineni, Jacques Y Roberge, Yalei Liu, R Michael Lawrence, James R Corte, Wu Yang, Mark Bednarz, John K Dickson, Zhengping Ma, Ramakrishna Seethala, Jean H M Feyen.   

Abstract

A 3D quantitative structure-activity relationship study for inhibition of calcium-sensing receptor in the aryloxypropanolamine series predicted that these molecules adopt a U-shaped conformation with pi-stacking between the two aromatic rings. This hypothesis led to the discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines capable of antagonizing the calcium-sensing receptor with potency comparable to that of NPS-2143.

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Year:  2005        PMID: 16216508     DOI: 10.1016/j.bmcl.2005.08.095

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


  5 in total

1.  Metabolism-guided design of short-acting calcium-sensing receptor antagonists.

Authors:  James A Southers; Jonathan N Bauman; David A Price; Paul S Humphries; Gayatri Balan; John F Sagal; Tristan S Maurer; Yan Zhang; Robert Oliver; Michael Herr; David R Healy; Mei Li; Brendon Kapinos; Gwendolyn D Fate; Keith A Riccardi; Vishwas M Paralkar; Thomas A Brown; Amit S Kalgutkar
Journal:  ACS Med Chem Lett       Date:  2010-05-13       Impact factor: 4.345

2.  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

3.  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 4.  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

Review 5.  Extracellular Calcium Receptor as a Target for Glutathione and Its Derivatives.

Authors:  Thomas Goralski; Jeffrey L Ram
Journal:  Int J Mol Sci       Date:  2022-01-10       Impact factor: 5.923

  5 in total

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