1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1499-503. doi: 10.1016/j.bmcl.2009.01.008. Epub 2009 Jan 10.

Abstract

Optimisation of a series of 4-piperidinyltriazoles led to the identification of compound 28a which showed good whole cell antiviral activity, excellent selectivity over the hERG ion channel and complete oral absorption.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / therapeutic use
  • Butanes / chemical synthesis*
  • Butanes / pharmacokinetics
  • Butanes / therapeutic use
  • CCR5 Receptor Antagonists*
  • Caco-2 Cells
  • Cell Line
  • Dogs
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism*
  • Humans
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacokinetics
  • Piperidines / therapeutic use
  • Rats
  • Receptors, CCR5 / metabolism
  • Stereoisomerism
  • Triazoles / chemical synthesis

Substances

  • Anti-HIV Agents
  • Butanes
  • CCR5 Receptor Antagonists
  • Piperidines
  • Receptors, CCR5
  • Triazoles