Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.
The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.
Lemoine
Rémy C
RC
Department of Medicinal Chemistry, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. remy_lemoine@yahoo.com
Petersen
Ann C
AC
Setti
Lina
L
Jekle
Andreas
A
Heilek
Gabrielle
G
deRosier
André
A
Ji
Changhua
C
Berry
Pamela
P
Rotstein
David M
DM
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D065100:CCR5 Receptor Antagonists; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D019713:Receptors, CCR5 / Q000378:metabolism; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D011720:Pyrazoles; D019713:Receptors, CCR5