Literature DB >> 15026036

Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists.

Shelley Allen1, Bradley Newhouse, Aaron S Anderson, Benjamin Fauber, Andrew Allen, David Chantry, Christine Eberhardt, Joshua Odingo, Laurence E Burgess.   

Abstract

Substituted thiazolidinones were identified as CCR4 antagonists from high throughput screening. Subsequent lead optimization efforts resulted in defined structure-activity relationships and the identification of potent antagonists (compounds 90 and 91) that inhibited the chemotaxis of Th2 T-cells in vitro.

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Year:  2004        PMID： 15026036     DOI： 10.1016/j.bmcl.2004.01.072

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


  7 in total

1.  SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor.

Authors:  Kazuyuki Hirata; Masayuki Kotoku; Noriyoshi Seki; Takaki Maeba; Katsuya Maeda; Shintaro Hirashima; Takayuki Sakai; Shingo Obika; Akimi Hori; Yasunori Hase; Takayuki Yamaguchi; Yoshiaki Katsuda; Takahiro Hata; Naoki Miyagawa; Kojo Arita; Yukihiro Nomura; Kota Asahina; Yusuke Aratsu; Masafumi Kamada; Tsuyoshi Adachi; Masato Noguchi; Satoki Doi; Paul Crowe; Erin Bradley; Ruo Steensma; Haiyan Tao; Morgan Fenn; Robert Babine; Xiaolin Li; Scott Thacher; Hiromasa Hashimoto; Makoto Shiozaki
Journal:  ACS Med Chem Lett       Date:  2015-11-04       Impact factor: 4.345

2.  Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.

Authors:  Nicholas Kindon; Glen Andrews; Andrew Baxter; David Cheshire; Paul Hemsley; Timothy Johnson; Yu-Zhen Liu; Dermot McGinnity; Mark McHale; Antonio Mete; James Reuberson; Bryan Roberts; John Steele; Barry Teobald; John Unitt; Deborah Vaughan; Iain Walters; Michael J Stocks
Journal:  ACS Med Chem Lett       Date:  2017-09-01       Impact factor: 4.345

3.  Distinct conformations of the chemokine receptor CCR4 with implications for its targeting in allergy.

Authors:  Jonathan M Viney; David P Andrew; Rhian M Phillips; Andrea Meiser; Pallavi Patel; Melissa Lennartz-Walker; David J Cousins; Nicholas P Barton; David A Hall; James E Pease
Journal:  J Immunol       Date:  2014-02-21       Impact factor: 5.422

4.  Screening of chemokine receptor CCR4 antagonists by capillary zone electrophoresis.

Authors:  Zhe Sun; Lin-Jie Tian; Qian Lin; Xiao-Mei Ling; Jun-Hai Xiao; Ying Wang
Journal:  J Pharm Anal       Date:  2011-10-21

5.  Toward the discovery of vaccine adjuvants: coupling in silico screening and in vitro analysis of antagonist binding to human and mouse CCR4 receptors.

Authors:  Matthew N Davies; Jagadeesh Bayry; Elma Z Tchilian; Janakiraman Vani; Melkote S Shaila; Emily K Forbes; Simon J Draper; Peter C L Beverley; David F Tough; Darren R Flower
Journal:  PLoS One       Date:  2009-11-30       Impact factor: 3.240

6.  New drugs targeting Th2 lymphocytes in asthma.

Authors:  Gaetano Caramori; David Groneberg; Kazuhiro Ito; Paolo Casolari; Ian M Adcock; Alberto Papi
Journal:  J Occup Med Toxicol       Date:  2008-02-27       Impact factor: 2.646

7.  Synthesis and antimicrobial activities of 5-Arylidene-thiazolidine-2,4-dione derivatives.

Authors:  Ivanildo Mangueira da Silva; João da Silva Filho; Priscila Brandão Gomes da Silva Santiago; Micalyne Soares do Egito; Carlos André de Souza; Frederico Leite Gouveia; Rafael Matos Ximenes; Kêsia Xisto da Fonseca Ribeiro de Sena; Antonio Rodolfo de Faria; Dalci José Brondani; Julianna Ferreira Cavalcanti de Albuquerque
Journal:  Biomed Res Int       Date:  2014-05-07       Impact factor: 3.411
  7 in total

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