Literature DB >> 18614364

Discovery of imidazole carboxamides as potent and selective CCK1R agonists.

Cheng Zhu1, Alexa R Hansen, Thomas Bateman, Zhesheng Chen, Tom G Holt, James A Hubert, Bindhu V Karanam, Susan J Lee, Jie Pan, Su Qian, Vijay B G Reddy, Marc L Reitman, Alison M Strack, Vincent Tong, Drew T Weingarth, Michael S Wolff, Doug J MacNeil, Ann E Weber, Joseph L Duffy, Scott D Edmondson.   

Abstract

High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.

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Year:  2008        PMID: 18614364     DOI: 10.1016/j.bmcl.2008.06.057

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


  7 in total

1.  Imidazole-derived agonists for the neurotensin 1 receptor.

Authors:  Paul M Hershberger; Michael P Hedrick; Satyamaheshwar Peddibhotla; Arianna Mangravita-Novo; Palak Gosalia; Yujie Li; Wilson Gray; Michael Vicchiarelli; Layton H Smith; Thomas D Y Chung; James B Thomas; Marc G Caron; Anthony B Pinkerton; Lawrence S Barak; Gregory P Roth
Journal:  Bioorg Med Chem Lett       Date:  2013-11-21       Impact factor: 2.823

2.  Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.

Authors:  Aditya J Desai; Brad R Henke; Laurence J Miller
Journal:  Bioorg Med Chem Lett       Date:  2015-03-24       Impact factor: 2.823

Review 3.  Cholecystokinin-induced satiety, a key gut servomechanism that is affected by the membrane microenvironment of this receptor.

Authors:  A J Desai; M Dong; K G Harikumar; L J Miller
Journal:  Int J Obes Suppl       Date:  2016-11-16

4.  Screening for positive allosteric modulators of cholecystokinin type 1 receptor potentially useful for management of obesity.

Authors:  Daniela G Dengler; Qing Sun; Kaleeckal G Harikumar; Laurence J Miller; Eduard A Sergienko
Journal:  SLAS Discov       Date:  2022-07-16       Impact factor: 3.341

5.  A type 1 cholecystokinin receptor mutant that mimics the dysfunction observed for wild type receptor in a high cholesterol environment.

Authors:  Aditya J Desai; Kaleeckal G Harikumar; Laurence J Miller
Journal:  J Biol Chem       Date:  2014-05-13       Impact factor: 5.157

Review 6.  Roles of Cholecystokinin in the Nutritional Continuum. Physiology and Potential Therapeutics.

Authors:  Laurence J Miller; Kaleeckal G Harikumar; Denise Wootten; Patrick M Sexton
Journal:  Front Endocrinol (Lausanne)       Date:  2021-06-02       Impact factor: 5.555

7.  Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays.

Authors:  Nisha S Sipes; Matthew T Martin; Parth Kothiya; David M Reif; Richard S Judson; Ann M Richard; Keith A Houck; David J Dix; Robert J Kavlock; Thomas B Knudsen
Journal:  Chem Res Toxicol       Date:  2013-05-16       Impact factor: 3.739

  7 in total

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