Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.
Elaboration of our previously disclosed spiropiperidine template led to the development of a series of novel CCR5 antagonists. Results of SAR exploration and preliminary lead characterization are described.
Rotstein
David M
DM
Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. david.rotstein@comcast.net
Gabriel
Stephen D
SD
Manser
Nicole
N
Filonova
Lubov
L
Padilla
Fernando
F
Sankuratri
Surya
S
Ji
Changhua
C
deRosier
Andre
A
Dioszegi
Marianna
M
Heilek
Gabrielle
G
Jekle
Andreas
A
Weller
Paul
P
Berry
Pamela
P
D000818:Animals; D065100:CCR5 Receptor Antagonists; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D065100:CCR5 Receptor Antagonists; D048289:Imidazolidines