306296-62-8Relevant academic research and scientific papers
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
McCombie, Stuart W.,Tagat, Jayaram R.,Vice, Susan F.,Lin, Sue-Ing,Steensma, Ruo,Palani, Anandan,Neustadt, Bernard R.,Baroudy, Bahige M.,Strizki, Julie M.,Endres, Michael,Cox, Kathleen,Dan, Niya,Chou, Chuan-Chu
, p. 567 - 571 (2007/10/03)
The unsymmetrical nicotinamide-N-oxide moiety in compound 1 was replaced with symmetrical isonicotinamides as well as 4,6-dimethyl pyrimidine-5-carboxamides. Compound 16 from the latter set reduced the number of rotamers, improved potency of inhibiting UIV entry, slightly diminished the affinity for the muscarine receptors and showed very good oral absorption.
Piperazine derivatives useful as CCR5 antagonists
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Page column 86, (2010/02/05)
The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1is hydrogen or alkyl; R2is substituted phenyl, substituted heter
