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Enhancing activity and selectivity in a series of pyrrol-1-yl-1-hydroxypyrazole-based aldose reductase inhibitors: The case of trifluoroacetylation.

Abstract:

Aldose reductase (ALR2) has been the target of therapeutic intervention for over 40 years; first, for its role in long-term diabetic complications and more recently as a key mediator in inflammation and cancer. However, efforts to prepare small-molecule aldose reductase inhibitors (ARIs) have mostly yielded carboxylic acids with rather poor pharmacokinetics. To address this limitation, the 1-hydroxypyrazole moiety has been previously established as a bioisostere of acetic acid in a group of a...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted manuscript

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Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Role:
Author
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Publisher:
Elsevier Publisher's website
Journal:
European Journal of Medicinal Chemistry Journal website
Volume:
130
Pages:
328-335
Publication date:
2017-02-24
Acceptance date:
2017-02-20
DOI:
EISSN:
1768-3254
ISSN:
0223-5234
Pubs id:
pubs:684099
URN:
uri:6ddd830b-bd37-4426-b2a6-7f964bf98d92
UUID:
uuid:6ddd830b-bd37-4426-b2a6-7f964bf98d92
Local pid:
pubs:684099

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