title: Combinatorial synthesis of CCR5 antagonists.
abstract: Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor. A potent CCR5 antagonist from the library, compound 11 was found to have moderate anti-HIV-1 activity.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. christopher_willoughby@merck.com
authors.forename: C A
authors.initials: CA
authors.lastname: Willoughby
authors.forename: S C
authors.initials: SC
authors.lastname: Berk
authors.forename: K G
authors.initials: KG
authors.lastname: Rosauer
authors.forename: S
authors.initials: S
authors.lastname: Degrado
authors.forename: K T
authors.initials: KT
authors.lastname: Chapman
authors.forename: S L
authors.initials: SL
authors.lastname: Gould
authors.forename: M S
authors.initials: MS
authors.lastname: Springer
authors.forename: L
authors.initials: L
authors.lastname: Malkowitz
authors.forename: W A
authors.initials: WA
authors.lastname: Schleif
authors.forename: D
authors.initials: D
authors.lastname: Hazuda
authors.forename: M
authors.initials: M
authors.lastname: Miller
authors.forename: J
authors.initials: J
authors.lastname: Kessler
authors.forename: R
authors.initials: R
authors.lastname: Danzeisen
authors.forename: K
authors.initials: K
authors.lastname: Holmes
authors.forename: J
authors.initials: J
authors.lastname: Lineberger
authors.forename: A
authors.initials: A
authors.lastname: Carella
authors.forename: G
authors.initials: G
authors.lastname: Carver
authors.forename: E A
authors.initials: EA
authors.lastname: Emini
mesh_terms: D065100:CCR5 Receptor Antagonists; D020650:Combinatorial Chemistry Techniques; D015497:HIV-1 / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D065100:CCR5 Receptor Antagonists