Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides

…, JW Clader, WJ Greenlee, S Vice, S McCombie…

Index: Palani, Anandan; Shapiro, Sherry; Clader, John W.; Greenlee, William J.; Vice, Susan; McCombie, Stuart; Cox, Kathleen; Strizki, Julie; Baroudy, Bahige M. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 4 p. 709 - 712

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Citation Number: 44

Abstract

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.