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Highly potent macro...
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Sandgren, VeronicaLinköpings universitet,Organisk Kemi,Tekniska högskolan
(author)
Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core : Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes
- Article/chapterEnglish2012
Publisher, publication year, extent ...
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Elsevier,2012
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electronicrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:liu-76172
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https://urn.kb.se/resolve?urn=urn:nbn:se:liu:diva-76172URI
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https://doi.org/10.1016/j.bmc.2012.05.039DOI
Supplementary language notes
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Language:English
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Summary in:English
Part of subdatabase
Classification
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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On the day of the defence day the status of this article was Manuscript.
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A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymatic and cell-based assays, were observed in this series of target compounds, with the best candidates displaying cell-based IC50 values in the low nanomolar range. As an attempt to improve potency, a phenyl substituent aiming at the S3 subpocket was introduced in the macrocyclic ring. X-ray analyses were performed on selected compounds, and enzyme-inhibitor interactions are discussed.
Subject headings and genre
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Alzheimer’s disease; BACE-1 inhibition; Macrocycles; Hydroxyethylamine (HEA) isostere
Added entries (persons, corporate bodies, meetings, titles ...)
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Agback, TatianaMedivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
(author)
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Johansson, Per-OlaMedivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
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Lindberg, JimmyMedivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
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Kvarnström, IngemarLinköpings universitet,Organisk Kemi,Tekniska högskolan(Swepub:liu)ingkv34
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Samuelsson, BertilMedivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
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Belda, OscarMedivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
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Dahlgren, AndersLinköpings universitet,Organisk Kemi,Tekniska högskolan(Swepub:liu)andda41
(author)
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Linköpings universitetOrganisk Kemi
(creator_code:org_t)
Related titles
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In:Bioorganic & Medicinal Chemistry: Elsevier29:14, s. 4377-43890968-08961464-3391
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