Endothiopeptide inhibitors of HIV-1 protease.
Endothiopeptide inhibitors of HIV-1 protease were synthesized by chemical and enzymatic methods to individually replace each backbone amide bond in 1 with a thioamide-linkage. Interestingly, agent 7, which contains a thioamide-linkage between the P2' and P3' positions of 1, was the most potent, competitive inhibitor of HIV-1 protease with a Ki of 3.4 microM.
Yao
S
S
Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Zutshi
R
R
Chmielewski
J
J
D002851:Chromatography, High Pressure Liquid; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D013854:Thioamides
D017320:HIV Protease Inhibitors; D009842:Oligopeptides; D013854:Thioamides