Synthesis and activity of pseudotripeptide inhibitors of HIV-1 protease containing D(-)-O-(benzyl)tartaric acid.
Four HIV-1 protease inhibitors containing [(S,S)-O-(benzyl) tartaric acid]-Pro as a transition-state mimic were prepared and evaluated by a spectrophotometric assay. Two pseudotripeptide derivatives showed weak inhibitory activity similar to acetylpepstatin.
Marastoni
M
M
Department of Pharmaceutical Science, University of Ferrara, Italy.
Fantin
G
G
Bortolotti
F
F
Tomatis
R
R
D000596:Amino Acids / Q000032:analysis; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013644:Tartrates / Q000138:chemical synthesis* / Q000494:pharmacology
D000596:Amino Acids; D017320:HIV Protease Inhibitors; D009842:Oligopeptides; D013644:Tartrates; C073513:KNI 102