Literature DB >> 21398122

Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.

Renato Skerlj1, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Jonathan Langille, Maria Di Fluri, David Bogucki, Wen Yang, Tongshuang Li, Letian Wang, Susan Nan, Ian Baird, Markus Metz, Marilyn Darkes, Jean Labrecque, Gloria Lau, Simon Fricker, Dana Huskens, Dominique Schols.   

Abstract

A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21398122     DOI： 10.1016/j.bmcl.2011.02.058

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


  2 in total

1.  Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.

Authors:  Renato Skerlj; Gary Bridger; Yuanxi Zhou; Elyse Bourque; Ernest McEachern; Sanjay Danthi; Jonathan Langille; Curtis Harwig; Duane Veale; Bryon Carpenter; Tuya Ba; Michael Bey; Ian Baird; Trevor Wilson; Markus Metz; Ron MacFarland; Renee Mosi; Veronique Bodart; Rebecca Wong; Simon Fricker; Dana Huskens; Dominique Schols
Journal:  ACS Med Chem Lett       Date:  2012-01-25       Impact factor: 4.345

Review 2.  CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV.

Authors:  Michelle B Kim; Kyle E Giesler; Yesim A Tahirovic; Valarie M Truax; Dennis C Liotta; Lawrence J Wilson
Journal:  Expert Opin Investig Drugs       Date:  2016-12       Impact factor: 6.206
  2 in total

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