title: Kynostatin (KNI)-227 and -272, highly potent anti-HIV agents: conformationally constrained tripeptide inhibitors of HIV protease containing allophenylnorstatine.
abstract: Selective and potent HIV protease inhibitors containing allophenylnorstatine [Apns; (2S, 3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition-state mimic were designed and synthesized. Among them, conformationally constrained tripeptide derivatives, kynostatin (KNI)-227 and -272 (Fig. 1), exhibited highly potent antiviral activities against a wide spectrum of HIV isolates. Ready availability due to the simple synthetic procedure and the excellent antiviral properties indicate that KNI-227 and KNI-272 are promising candidates as selective anti-AIDS drugs.
authors.affiliation: Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Mimoto
authors.forename: J
authors.initials: J
authors.lastname: Imai
authors.forename: S
authors.initials: S
authors.lastname: Kisanuki
authors.forename: H
authors.initials: H
authors.lastname: Enomoto
authors.forename: N
authors.initials: N
authors.lastname: Hattori
authors.forename: K
authors.initials: K
authors.lastname: Akaji
authors.forename: Y
authors.initials: Y
authors.lastname: Kiso
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D017320:HIV Protease Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D009842:Oligopeptides; C077823:kynostatin 227; C077822:kynostatin 272