Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
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.
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)
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: Synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides
The synthesis, SAR and biological evaluation of symmetrical amide analogues of our clinical candidate SCH 351125 are described. A series of potent and orally bioavailable CCR5 antagonists containing symmetrical 2,6-dimethyl isonicotinamides and 2, 6-dimethyl pyrimidines amides were generated with enhanced affinity for the CCR5 receptor.
Palani, Anandan,Shapiro, Sherry,Clader, John W.,Greenlee, William J.,Vice, Susan,McCombie, Stuart,Cox, Kathleen,Strizki, Julie,Baroudy, Bahige M.
p. 709 - 712
(2007/10/03)
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