1.
Bioorg Med Chem Lett
; 19(5): 1499-503, 2009 Mar 01.
Article
in English
| MEDLINE
| ID: mdl-19185490
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.
Subject(s)
Anti-HIV Agents/chemical synthesis , Butanes/chemical synthesis , CCR5 Receptor Antagonists , HIV Infections/drug therapy , HIV Infections/metabolism , Piperidines/chemical synthesis , Animals , Anti-HIV Agents/therapeutic use , Butanes/pharmacokinetics , Butanes/therapeutic use , Caco-2 Cells , Cell Line , Dogs , Humans , Piperidines/pharmacokinetics , Piperidines/therapeutic use , Rats , Receptors, CCR5/metabolism , Stereoisomerism , Triazoles/chemical synthesis
2.
Bioorg Med Chem Lett
; 19(4): 1075-9, 2009 Feb 15.
Article
in English
| MEDLINE
| ID: mdl-19171484
ABSTRACT
The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak activity at the hERG ion channel.