title: Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.
abstract: The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.
authors.affiliation: Department of Medicinal Chemistry, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. remy_lemoine@yahoo.com
authors.forename: Rémy C
authors.initials: RC
authors.lastname: Lemoine
authors.forename: Ann C
authors.initials: AC
authors.lastname: Petersen
authors.forename: Lina
authors.initials: L
authors.lastname: Setti
authors.forename: Andreas
authors.initials: A
authors.lastname: Jekle
authors.forename: Gabrielle
authors.initials: G
authors.lastname: Heilek
authors.forename: André
authors.initials: A
authors.lastname: deRosier
authors.forename: Changhua
authors.initials: C
authors.lastname: Ji
authors.forename: Pamela
authors.initials: P
authors.lastname: Berry
authors.forename: David M
authors.initials: DM
authors.lastname: Rotstein
mesh_terms: 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
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D011720:Pyrazoles; D019713:Receptors, CCR5