1287211-78-2Relevant academic research and scientific papers
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series
Wanner, Jutta,Chen, Lijing,Lemoine, Rémy C.,Kondru, Rama,Jekle, Andreas,Heilek, Gabrielle,Derosier, André,Ji, Changhua,Berry, Pamela W.,Rotstein, David M.
, p. 6802 - 6807 (2010)
Replacement of a secondary amide with a piperidine or azetidine moiety in a series of CCR5 antagonists led to the discovery of compounds with increased intrinsic permeability. This effort led to the identification of a potent CCR5 antagonist which exhibited an improved in vivo pharmacokinetic profile.
