Literature DB >> 16242326

Synthesis of the PPARbeta/delta-selective agonist GW501516 and C4-thiazole-substituted analogs.

Raquel Pereira1, Claudine Gaudon, Beatriz Iglesias, Pierre Germain, Hinrich Gronemeyer, Angel R de Lera.   

Abstract

Sequential, position-selective, Pd-catalyzed cross-coupling reactions of 2,4-dibromo-5-hydroxymethylthiazole provided the scaffold for the synthesis of GW501516, the most potent PPARbeta/delta agonist yet described, and equally selective analogs at the thiazole-C4 position.

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Year:  2005        PMID: 16242326     DOI: 10.1016/j.bmcl.2005.09.060

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


  5 in total

1.  Inhibition of IκB kinase-β and IκB kinase-α by heterocyclic adamantyl arotinoids.

Authors:  José García-Rodríguez; Santiago Pérez-Rodríguez; María A Ortiz; Raquel Pereira; Angel R de Lera; F Javier Piedrafita
Journal:  Bioorg Med Chem       Date:  2014-01-10       Impact factor: 3.641

2.  A new strategy for the synthesis of β-benzylmercaptoethylamine derivatives.

Authors:  Subrata Ghosh; Gregory P Tochtrop
Journal:  Tetrahedron Lett       Date:  2009-04       Impact factor: 2.415

3.  Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Authors:  Joshua Almond-Thynne; David C Blakemore; David C Pryde; Alan C Spivey
Journal:  Chem Sci       Date:  2016-08-09       Impact factor: 9.825

4.  Enantioselective Synthesis of a Novel Thiazoline Core as a Potent Peroxisome Proliferator-Activated Receptor δ Agonist.

Authors:  Su-Jeong Lee; Mallesham Samala; Seo Yeon Woo; Dongyup Hahn; Dayoung Kim; Tara Man Kadayat; Kyungjin Jung; Jina Kim; Dong-Su Kim; Sugyeong Kwon; Shinae Kim; Kyung-Hee Kim; Sang-Jip Nam; Sung Jin Cho; Jungwook Chin
Journal:  ACS Omega       Date:  2018-02-15

5.  Structure-based virtual screening and discovery of New PPARδ/γ dual agonist and PPARδ and γ agonists.

Authors:  Vinicius G Maltarollo; Marie Togashi; Alessandro S Nascimento; Kathia M Honorio
Journal:  PLoS One       Date:  2015-03-13       Impact factor: 3.240

  5 in total

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