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Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic
Uppsala University.
Uppsala University.
Uppsala University.
Linköping University, Department of Physics, Chemistry and Biology, Organic Chemistry . Linköping University, The Institute of Technology.
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2009 (English)In: BIOORGANIC and MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, Vol. 19, no 16, 4711-4714 p.Article in journal (Refereed) Published
Abstract [en]

Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC50 value of 0.23 mu M.

Place, publisher, year, edition, pages
2009. Vol. 19, no 16, 4711-4714 p.
Keyword [en]
Alzheimers disease, BACE-1, Enzyme inhibitor, Transition state mimetic
National Category
Medical and Health Sciences
URN: urn:nbn:se:liu:diva-19803DOI: 10.1016/j.bmcl.2009.06.065OAI: diva2:229059
Available from: 2009-08-11 Created: 2009-08-10 Last updated: 2009-08-11

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Rosenquist, Åsa
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Organic Chemistry The Institute of Technology
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