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

Christopher G Barber; David C Blakemore; Jean-Yves Chiva; Rachel L Eastwood; Donald S Middleton; Kerry A Paradowski

doi:10.1016/j.bmcl.2009.01.008

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.

Authors

Christopher G Barber¹, David C Blakemore, Jean-Yves Chiva, Rachel L Eastwood, Donald S Middleton, Kerry A Paradowski

Affiliation

¹ Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.

PMID: 19185490
DOI: 10.1016/j.bmcl.2009.01.008

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