Design and synthesis of hydroxyethylene-based BACE-1 inhibitors incorporating extended P1 substituents
2013 (English)In: Open Medicinal Chemistry Journal, ISSN 1874-1045, Vol. 7, 1-15 p.Article in journal (Refereed) Published
Novel BACE-1 inhibitors with a hydroxyethylene central core have been developed. Modified P1´ and extended P1 substituents were incorporated with the aim to explore potential interactions with the S1´ and the S1-S3 pocket, respectively, of BACE-1. Inhibitors were identified displaying IC50 values in the nanomolar range, i.e., 69 nM for the most potent compound. Possible inhibitor interactions with the enzyme are also discussed.
Place, publisher, year, edition, pages
Bussum, Netherlands: Bentham Open , 2013. Vol. 7, 1-15 p.
IdentifiersURN: urn:nbn:se:liu:diva-76171DOI: 10.2174/1874104501307010001OAI: oai:DiVA.org:liu-76171DiVA: diva2:512914