Synthesis and evaluation of a new class of tertiary alcohol based BACE-1 inhibitors
2009 (English)In: Tetrahedron, ISSN 0040-4020, E-ISSN 1464-5416, Vol. 65, no 48, 10047-10059 p.Article in journal (Refereed) Published
BACE-1 has emerged as one of the best characterized targets for future Alzheimer therapy. In accordance with the successful identification of masked inhibitors of HIV-1 protease, we envisioned that tert-alcohol containing transition-state mimicking structures would also be worthwhile evaluating as BACE-1 inhibitors. Twelve novel inhibitors were prepared via synthetic routes using epoxyalcohol derivates as key intermediates. The best synthesized tert-hydroxy inhibitor exhibited a BACE-1 IC50 value of 0.38 mu M.
Place, publisher, year, edition, pages
2009. Vol. 65, no 48, 10047-10059 p.
Alzheimer's disease, BACE-1 inhibitors, Transitions state isostere
IdentifiersURN: urn:nbn:se:uu:diva-109024DOI: 10.1016/j.tet.2009.09.106ISI: 000271841700018OAI: oai:DiVA.org:uu-109024DiVA: diva2:242284