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P2 '-truncated BACE...
P2 '-truncated BACE-1 inhibitors with a novel hydroxethylene-like core
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- Adrian Meredith, Jenny, 1971- (author)
- Stockholms universitet,Institutionen för organisk kemi,Bertil Samuelsson
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- Björklund, Catarina, 1981- (author)
- Stockholms universitet,Institutionen för organisk kemi,Bertil Samuelsson
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- Adolfsson, Hans (author)
- Stockholms universitet,Institutionen för organisk kemi,Hans Adolfsson
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Jansson, Katarina (author)
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- Hallberg, Anders (author)
- Uppsala universitet,Institutionen för läkemedelskemi,Institutionen för läkemedelskemi, Uppsala universitet
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Rosenquist, Åsa (author)
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- Samuelsson, Bertil (author)
- Stockholms universitet,Institutionen för organisk kemi
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(creator_code:org_t)
- Elsevier BV, 2010
- 2010
- English.
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In: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234 .- 1768-3254. ; 45:2, s. 542-554
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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https://urn.kb.se/re...
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Abstract
Subject headings
Close
- Highly potent BACE-1 protease inhibitors derived from a novel hydroxyethylene-like core structure were recently developed by our group using X-ray crystal structure data and molecular modelling. In a continuation of this work guided by molecular modelling we have explored a truncated core motif where the P2' amide group is replaced by an ether linkage resulting in a set of alkoxy, aryloxy and alkylaryl groups, with the overall aim to reduce molecular weight and the number of amide bonds to increase permeability and bestow the inhibitors with drug-like features. The most potent of these inhibitors displayed a BACE-I IC50 value of 140 nM. The synthesis of these BACE-I inhibitors utilizes readily available starting materials, furnishing the target compounds in good overall yields.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- BACE-1
- BACE
- beta-Secretase
- Asp2
- Memapsin
- PI
- MEDICINE
- MEDICIN
- Pharmaceutical chemistry
- organisk kemi
Publication and Content Type
- ref (subject category)
- art (subject category)
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