1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2.
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.
Barber
Christopher G
CG
Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
Blakemore
David C
DC
Chiva
Jean-Yves
JY
Eastwood
Rachel L
RL
Middleton
Donald S
DS
Paradowski
Kerry A
KA
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D002073:Butanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D065100:CCR5 Receptor Antagonists; D018938:Caco-2 Cells; D002460:Cell Line; D004285:Dogs; D015658:HIV Infections / Q000188:drug therapy* / Q000378:metabolism*; D006801:Humans; D010880:Piperidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D019713:Receptors, CCR5 / Q000378:metabolism; D013237:Stereoisomerism; D014230:Triazoles / Q000138:chemical synthesis
D019380:Anti-HIV Agents; D002073:Butanes; D065100:CCR5 Receptor Antagonists; D010880:Piperidines; D019713:Receptors, CCR5; D014230:Triazoles