Literature DB >> 20363624

Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).

P Douglas Boatman1, Thomas O Schrader, Michelle Kasem, Benjamin R Johnson, Philip J Skinner, Jae-Kyu Jung, Jerry Xu, Martin C Cherrier, Peter J Webb, Graeme Semple, Carleton R Sage, Jens Knudsen, Ruoping Chen, Andrew K Taggart, Ester Carballo-Jane, Jeremy G Richman.   

Abstract

Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20363624     DOI: 10.1016/j.bmcl.2010.03.062

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


  6 in total

1.  Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain.

Authors:  Sangdon Han; Lars Thoresen; Jae-Kyu Jung; Xiuwen Zhu; Jayant Thatte; Michelle Solomon; Ibragim Gaidarov; David J Unett; Woo Hyun Yoon; Jeremy Barden; Abu Sadeque; Amin Usmani; Chuan Chen; Graeme Semple; Andrew J Grottick; Hussein Al-Shamma; Ronald Christopher; Robert M Jones
Journal:  ACS Med Chem Lett       Date:  2017-11-30       Impact factor: 4.345

2.  Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.

Authors:  Jun Qin; Ashwin Rao; Xiao Chen; Xiaohong Zhu; Zhidan Liu; Xianhai Huang; Sylvia Degrado; Ying Huang; Dong Xiao; Robert Aslanian; Boonlert Cheewatrakoolpong; Hongtao Zhang; Scott Greenfeder; Constance Farley; John Cook; Stan Kurowski; Qiu Li; Margaret van Heek; Madhu Chintala; Ganfeng Wang; Yunsheng Hsieh; Fangbiao Li; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2010-12-08       Impact factor: 4.345

3.  Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.

Authors:  Curt A Dvorak; Changlu Liu; Jonathan Shelton; Chester Kuei; Steven W Sutton; Timothy W Lovenberg; Nicholas I Carruthers
Journal:  ACS Med Chem Lett       Date:  2012-06-11       Impact factor: 4.345

4.  Measuring niacin-associated skin toxicity (NASTy) stigmata along with symptoms to aid development of niacin mimetics.

Authors:  Richard L Dunbar; Harsh Goel; Sony Tuteja; Wen-Liang Song; Grace Nathanson; Zeeshan Babar; Dusanka Lalic; Joel M Gelfand; Daniel J Rader; Gary L Grove
Journal:  J Lipid Res       Date:  2017-01-23       Impact factor: 5.922

Review 5.  Tetrazoles via Multicomponent Reactions.

Authors:  Constantinos G Neochoritis; Ting Zhao; Alexander Dömling
Journal:  Chem Rev       Date:  2019-02-01       Impact factor: 60.622

Review 6.  G protein-coupled receptors for energy metabolites as new therapeutic targets.

Authors:  Clara C Blad; Cong Tang; Stefan Offermanns
Journal:  Nat Rev Drug Discov       Date:  2012-07-13       Impact factor: 84.694

  6 in total

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