Literature DB >> 28642104

Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists.

Xuqing Zhang1, Chaozhong Cai2, Michael Winters2, Michele Wells2, Mark Wall2, James Lanter2, Zhihua Sui2, Jingyuan Ma3, Aaron Novack3, Imad Nashashibi3, Yuanping Wang2, Wen Yan2, Arthur Suckow2, Hong Hua2, Austin Bell2, Peter Haug2, Wilma Clapper2, Celia Jenkinson2, Joseph Gunnet2, James Leonard2, William V Murray2.   

Abstract

A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  GPR120; Phenylpropanoic acid; Type 2 diabetes

Mesh：

Substances：

Year:  2017        PMID： 28642104     DOI： 10.1016/j.bmcl.2017.06.028

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


  8 in total

1.  Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.

Authors:  Xuqing Zhang; Chaozhong Cai; Zhihua Sui; Mark Macielag; Yuanping Wang; Wen Yan; Arthur Suckow; Hong Hua; Austin Bell; Peter Haug; Wilma Clapper; Celia Jenkinson; Joseph Gunnet; James Leonard; William V Murray
Journal:  ACS Med Chem Lett       Date:  2017-07-27       Impact factor: 4.345

2.  Synthesis of 5-(Fluoroalkyl)isoxazole Building Blocks by Regioselective Reactions of Functionalized Halogenoximes.

Authors:  Bohdan A Chalyk; Kateryna V Hrebeniuk; Yulia V Fil; Konstantin S Gavrilenko; Alexander B Rozhenko; Bohdan V Vashchenko; Oleksandr V Borysov; Angelina V Biitseva; Pavlo S Lebed; Iulia Bakanovych; Yurii S Moroz; Oleksandr O Grygorenko
Journal:  J Org Chem       Date:  2019-10-30       Impact factor: 4.354

3.  GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.

Authors:  Gabriele Carullo; Sarah Mazzotta; Margarita Vega-Holm; Fernando Iglesias-Guerra; José Manuel Vega-Pérez; Francesca Aiello; Antonella Brizzi
Journal:  J Med Chem       Date:  2021-04-10       Impact factor: 7.446

4.  Pharmacokinetics of Panaxynol in Mice.

Authors:  Hossam Tashkandi; Anusha Chaparala; Sean Peng; Mitzi Nagarkatti; Prakash Nagarkatti; Alexander A Chumanevich; Lorne J Hofseth
Journal:  J Cancer Sci Clin Ther       Date:  2020-06-01

Review 5.  Pharmacology of Free Fatty Acid Receptors and Their Allosteric Modulators.

Authors:  Manuel Grundmann; Eckhard Bender; Jens Schamberger; Frank Eitner
Journal:  Int J Mol Sci       Date:  2021-02-10       Impact factor: 5.923

6.  Novel GPR120 Agonists with Improved Pharmacokinetic Profiles for the Treatment of Type 2 Diabetes.

Authors:  Guoxia Ji; Qinghua Guo; Qidi Xue; Ruifang Kong; Shiben Wang; Kang Lei; Renmin Liu; Xuekun Wang
Journal:  Molecules       Date:  2021-11-16       Impact factor: 4.411

Review 7.  Dissecting the Physiology and Pathophysiology of Glucagon-Like Peptide-1.

Authors:  Silvano Paternoster; Marco Falasca
Journal:  Front Endocrinol (Lausanne)       Date:  2018-10-11       Impact factor: 5.555

8.  Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers.

Authors:  Chao Wang; Yuelin Li; Zi Liu; Zeyu Wang; Zihan Liu; Shuai Man; Yujing Zhang; Kai Bao; Yingliang Wu; Qi Guan; Daiying Zuo; Weige Zhang
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051
  8 in total

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