Literature DB >> 22033460

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

Renato Skerlj1, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Ernest McEachern, Jonathan Langille, Curtis Harwig, Duane Veale, Wen Yang, Tongshong Li, Yongbao Zhu, Michael Bey, Ian Baird, Michael Sartori, Markus Metz, Renee Mosi, Kim Nelson, Veronique Bodart, Rebecca Wong, Simon Fricker, Ron Mac Farland, Dana Huskens, Dominique Schols.   

Abstract

A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics. Copyright Â
© 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 22033460     DOI: 10.1016/j.bmcl.2011.09.133

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


  3 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

3.  Discovery of Novel CCR5 Ligands as Anticolorectal Cancer Agents by Sequential Virtual Screening.

Authors:  Mariam A El-Zohairy; Darius P Zlotos; Martin R Berger; Hassan H Adwan; Yasmine M Mandour
Journal:  ACS Omega       Date:  2021-04-16
  3 in total

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