title: CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives.
abstract: High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Initial modifications of the guanylhydrazone series indicated that substitution of the benzyl group at the para-position was well tolerated. Substitution at the 5-position of the central phenyl ring was critical for potency. Replacement of the guanylhydrazone group led to the discovery of a novel series of CCR5 antagonists.
authors.affiliation: Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA.
authors.forename: Robert G
authors.initials: RG
authors.lastname: Wei
authors.forename: Damian O
authors.initials: DO
authors.lastname: Arnaiz
authors.forename: Yuo-Ling
authors.initials: YL
authors.lastname: Chou
authors.forename: Dave
authors.initials: D
authors.lastname: Davey
authors.forename: Laura
authors.initials: L
authors.lastname: Dunning
authors.forename: Wheeseong
authors.initials: W
authors.lastname: Lee
authors.forename: Shou-Fu
authors.initials: SF
authors.lastname: Lu
authors.forename: James
authors.initials: J
authors.lastname: Onuffer
authors.forename: Bin
authors.initials: B
authors.lastname: Ye
authors.forename: Gary
authors.initials: G
authors.lastname: Phillips
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry*; D065100:CCR5 Receptor Antagonists; D002478:Cells, Cultured; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D008935:Mitoguazone / Q000031:analogs & derivatives*; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D065100:CCR5 Receptor Antagonists; D008935:Mitoguazone