title: Synthesis and human immunodeficiency virus (HIV)-1 protease inhibitory activity of tripeptide analogues containing a dioxoethylene moiety.
abstract: Tripeptide analogues 2 and 3 containing a dioxoethylene moiety were designed based on the characteristic structure of the naturally occurring human immunodeficiency virus (HIV)-1 protease inhibitors RPI-856 A, B, C and D (1). The compounds (2, 3) prepared showed high inhibitory activity, comparable to that of RPI-856 A, against HIV-1 protease in vitro.
authors.affiliation: Pharmaceutical Research Laboratories III, Takeda Chemical Industries, Ltd., Osaka, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Kitazaki
authors.forename: T
authors.initials: T
authors.lastname: Asano
authors.forename: K
authors.initials: K
authors.lastname: Kato
authors.forename: S
authors.initials: S
authors.lastname: Kishimoto
authors.forename: K
authors.initials: K
authors.lastname: Itoh
mesh_terms: D055598:Chemical Phenomena; D002627:Chemistry, Physical; D016333:HIV Protease / Q000378:metabolism; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000201:enzymology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology
chemical_list: D017320:HIV Protease Inhibitors; D009842:Oligopeptides; C088529:RPI 856 A; C088530:RPI 856 C; D016333:HIV Protease