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Structural essentials for β-N-acetylhexosaminidase inhibition by amides of prolines, pipecolic and azetidine carboxylic acids

Abstract:

This paper explores the computer modelling aided design and synthesis of β-N-acetylhexosaminidase inhibitors along with their applicability to human disease treatment through biological evaluation in both an enzymatic and cellular setting. We investigated the importance of individual stereocenters, variations in structure-activity relationships along with factors influencing cell penetration. To achieve these goals we modified nitrogen heterocycles in terms of ring size, side chains present a...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/c6ob01549b

Authors


More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
Publisher:
Royal Society of Chemistry
Journal:
Organic & Biomolecular Chemistry More from this journal
Volume:
14
Issue:
44
Pages:
10371-10385
Publication date:
2016-10-06
Acceptance date:
2016-10-06
DOI:
EISSN:
1477-0539
ISSN:
1477-0520
Language:
English
Keywords:
Pubs id:
pubs:653196
UUID:
uuid:e1a8926c-936b-4abc-ab44-f4245de64426
Local pid:
pubs:653196
Source identifiers:
653196
Deposit date:
2016-11-01

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