title: Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
abstract: A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. 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 / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D065100:CCR5 Receptor Antagonists; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000302:isolation & purification; D006801:Humans; D006827:Hydantoins / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D006827:Hydantoins