Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic
2008 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, Vol. 51, no 4, 1053-1057 p.Article in journal (Refereed) Published
A new generation of HIV-1 protease inhibitors encompassing a tertiary-alcohol-based transition-state mimic has been developed. By elongation of the core structure of recently reported inhibitors with two carbon atoms and by varying the P1' group of the compounds, efficient inhibitors were obtained with Ki down to 2.3 nM and EC50 down to 0.17 microM. Two inhibitor-enzyme X-ray structures are reported.
Place, publisher, year, edition, pages
2008. Vol. 51, no 4, 1053-1057 p.
Medical and Health Sciences
IdentifiersURN: urn:nbn:se:uu:diva-102908DOI: 10.1021/jm070680hISI: 000253353800037PubMedID: 18215014OAI: oai:DiVA.org:uu-102908DiVA: diva2:216968