Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.
Lemoine
Rémy C
RC
Department of Medicinal Chemistry, Roche Palo Alto, Palo Alto, CA 94304, USA. remy.lemoine@roche.com
Petersen
Ann C
AC
Setti
Lina
L
Chen
Lijing
L
Wanner
Jutta
J
Jekle
Andreas
A
Heilek
Gabrielle
G
deRosier
André
A
Ji
Changhua
C
Rotstein
David M
DM
D065100:CCR5 Receptor Antagonists; D004353:Drug Evaluation, Preclinical; D008958:Models, Molecular; D010880:Piperidines / Q000737:chemistry*
C481395:4-aminopiperidine; D065100:CCR5 Receptor Antagonists; D010880:Piperidines