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Design and synthesi...
Design and synthesis of hydroxyethylene-based BACE-1 inhibitors incorporating extended P1 substituents
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- Sandgren, Veronica (author)
- Linköpings universitet,Organisk Kemi,Tekniska högskolan
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- Bäck, Marcus (author)
- Linköpings universitet,Organisk Kemi,Tekniska högskolan
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- Kvarnström, Ingemar (author)
- Linköpings universitet,Organisk Kemi,Tekniska högskolan
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- Dahlgren, Anders (author)
- Linköpings universitet,Organisk Kemi,Tekniska högskolan
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(creator_code:org_t)
- Bussum, Netherlands : Bentham Open, 2013
- 2013
- English.
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In: Open Medicinal Chemistry Journal. - Bussum, Netherlands : Bentham Open. - 1874-1045. ; 7, s. 1-15
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https://liu.diva-por... (primary) (Raw object)
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https://openmedicina...
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https://urn.kb.se/re...
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https://doi.org/10.2...
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Abstract
Subject headings
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- 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.
Publication and Content Type
- ref (subject category)
- art (subject category)
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