Literature DB >> 21776181

Feasible Synthesis of Antagonist of GPR40 by Constructing 2-Thiouracil Ring viaAcid Mediated Cyclization.

Yongfeng Zhao1, Yang Song, Xiulin Shen, Jiayu Liao.   

Abstract

GW1100 is an antagonist of GPR40 identified by high throughput screening recently. The synthesis of GW1100 has been developed. The key step involves cyclization of the 2-thiouracil heterocycle under acidic condition at room temperature.

Entities:  

Year:  2011        PMID： 21776181      PMCID： PMC3137925          DOI： 10.3987/COM-11-12175

Source DB:  PubMed          Journal:  Heterocycles        ISSN： 0385-5414            Impact factor:   0.831


  8 in total

1.  Synthesis and evaluation of a new series of substituted acyl(thio)urea and thiadiazolo [2,3-a] pyrimidine derivatives as potent inhibitors of influenza virus neuraminidase.

Authors:  Chuanwen Sun; Xiaodong Zhang; Hai Huang; Pei Zhou
Journal:  Bioorg Med Chem       Date:  2006-09-18       Impact factor: 3.641

2.  Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.

Authors:  Celia P Briscoe; Andrew J Peat; Stephen C McKeown; David F Corbett; Aaron S Goetz; Thomas R Littleton; David C McCoy; Terry P Kenakin; John L Andrews; Carina Ammala; James A Fornwald; Diane M Ignar; Stephen Jenkinson
Journal:  Br J Pharmacol       Date:  2006-05-15       Impact factor: 8.739

3.  n-Butyl 5-Chloro-2-pyrimidoxyacetate--a Plant Growth Regulator Analog.

Authors:  D G Crosby; A J Vlitos
Journal:  Science       Date:  1958-08-29       Impact factor: 47.728

4.  Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.

Authors:  Fabrizio Micheli; Alessandra Pasquarello; Giovanna Tedesco; Dieter Hamprecht; Giorgio Bonanomi; Anna Checchia; Albert Jaxa-Chamiec; Federica Damiani; Silvia Davalli; Daniele Donati; Chiara Gallotti; Marcella Petrone; Marilisa Rinaldi; Graham Riley; Silvia Terreni; Martyn Wood
Journal:  Bioorg Med Chem Lett       Date:  2006-05-30       Impact factor: 2.823

5.  Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.

Authors:  Yasuaki Itoh; Yuji Kawamata; Masataka Harada; Makoto Kobayashi; Ryo Fujii; Shoji Fukusumi; Kazuhiro Ogi; Masaki Hosoya; Yasuhiro Tanaka; Hiroshi Uejima; Hideyuki Tanaka; Minoru Maruyama; Rie Satoh; Shoichi Okubo; Hideki Kizawa; Hidetoshi Komatsu; Fumika Matsumura; Yuko Noguchi; Tokuyuki Shinohara; Shuji Hinuma; Yukio Fujisawa; Masahiko Fujino
Journal:  Nature       Date:  2003-02-23       Impact factor: 49.962

6.  The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse.

Authors:  Pär Steneberg; Nir Rubins; Reut Bartoov-Shifman; Michael D Walker; Helena Edlund
Journal:  Cell Metab       Date:  2005-04       Impact factor: 27.287

7.  Synthesis of functionalized diarylmethanes via a copper-catalyzed cross-coupling of arylmagnesium reagents with benzylic phosphates.

Authors:  Christiane C Kofink; Paul Knochel
Journal:  Org Lett       Date:  2006-08-31       Impact factor: 6.005

8.  Total synthesis of pinnamine and anatoxin-a via a common intermediate. A caveat on the anatoxin-a endgame.

Authors:  Thomas Hjelmgaard; Inger Søtofte; David Tanner
Journal:  J Org Chem       Date:  2005-07-08       Impact factor: 4.354
  8 in total
  2 in total

Review 1.  Activation of GPR40 as a therapeutic target for the treatment of type 2 diabetes.

Authors:  Charles F Burant
Journal:  Diabetes Care       Date:  2013-08       Impact factor: 19.112

Review 2.  Pharmacology and physiology of gastrointestinal enteroendocrine cells.

Authors:  O J Mace; B Tehan; F Marshall
Journal:  Pharmacol Res Perspect       Date:  2015-07-07
  2 in total

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