title: Solid-phase syntheses of olefin-containing inhibitors for HTLV-1 protease using the Horner-Emmons reaction.
abstract: [reaction: see text] The solid-phase Horner-Emmons reaction was successfully applied for the convenient syntheses of olefin-containing protease inhibitors. The isomerization during the solid-phase Horner-Emmons reaction can be minimized simply by the use of an appropriate amount of the base. The synthesized olefin peptides, which have an olefin gamma-amino acid at the scissile site, were found to act as effective inhibitors for the HTLV-1 protease for the first time.
authors.affiliation: Institute for Protein Research, Osaka University, 3-2 Yamadaoka, Suita, Osaka 565-0871, Japan.
authors.forename: Jeong Kyu
authors.initials: JK
authors.lastname: Bang
authors.forename: Hiromi
authors.initials: H
authors.lastname: Naka
authors.forename: Kenta
authors.initials: K
authors.lastname: Teruya
authors.forename: Saburo
authors.initials: S
authors.lastname: Aimoto
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Konno
authors.forename: Kazuto
authors.initials: K
authors.lastname: Nosaka
authors.forename: Tadashi
authors.initials: T
authors.lastname: Tatsumi
authors.forename: Kenichi
authors.initials: K
authors.lastname: Akaji
mesh_terms: D000475:Alkenes / Q000737:chemistry*; D000595:Amino Acid Sequence; D020650:Combinatorial Chemistry Techniques; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis*; D020128:Inhibitory Concentration 50; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000475:Alkenes; D017320:HIV Protease Inhibitors; D009842:Oligopeptides