title: Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.
abstract: Replacement of the large hydantoin-indole moiety from our previous work with a variety of smaller heterocyclic analogues gave rise to potent CCR5 antagonists having binding affinity comparable to the hydantoin analogues. The synthesis, SAR, and biological profiles of this class of antagonists are described.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, RY 121-240, PO Box 2000, Rahway, NJ 07065, USA. dooseop_kim@merck.com
authors.forename: D
authors.initials: D
authors.lastname: Kim
authors.forename: L
authors.initials: L
authors.lastname: Wang
authors.forename: C G
authors.initials: CG
authors.lastname: Caldwell
authors.forename: P
authors.initials: P
authors.lastname: Chen
authors.forename: P E
authors.initials: PE
authors.lastname: Finke
authors.forename: B
authors.initials: B
authors.lastname: Oates
authors.forename: M
authors.initials: M
authors.lastname: MacCoss
authors.forename: S G
authors.initials: SG
authors.lastname: Mills
authors.forename: L
authors.initials: L
authors.lastname: Malkowitz
authors.forename: S L
authors.initials: SL
authors.lastname: Gould
authors.forename: J A
authors.initials: JA
authors.lastname: DeMartino
authors.forename: M S
authors.initials: MS
authors.lastname: Springer
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: G
authors.initials: G
authors.lastname: Carver
authors.forename: A
authors.initials: A
authors.lastname: Carella
authors.forename: K
authors.initials: K
authors.lastname: Holmes
authors.forename: J
authors.initials: J
authors.lastname: Lineberger
authors.forename: W A
authors.initials: WA
authors.lastname: Schleif
authors.forename: E A
authors.initials: EA
authors.lastname: Emini
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D065100:CCR5 Receptor Antagonists; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000302:isolation & purification; D006367:HeLa Cells; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D006571:Heterocyclic Compounds