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Journal article

Design, synthesis, and biological evaluation of novel indoles targeting the influenza PB2 cap binding region

Abstract:

In the search for novel influenza inhibitors we evaluated 7-fluoro-substituted indoles as bioisosteric replacements for the 7-azaindole scaffold of Pimodivir, a PB2 (polymerase basic protein 2) inhibitor currently in clinical development. Specifically, a 5,7-difluoroindole derivative 11a was identified as a potent and metabolically stable influenza inhibitor. 11a demonstrated a favorable oral pharmacokinetic profile and in vivo efficacy in mice. In addition, it was found that 11a was not at r...

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Publication status:
Published
Peer review status:
Peer reviewed

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Role:
Author
ORCID:
0000-0002-3759-6771
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Role:
Author
ORCID:
0000-0003-2880-2534
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Division:
MSD
Department:
NDM
Subgroup:
Structural Biology
Role:
Author
ORCID:
0000-0003-0159-9257
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of medicinal chemistry Journal website
Volume:
62
Issue:
21
Pages:
9680-9690
Place of publication:
United States
Publication date:
2019-10-24
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pmid:
31647875
Pubs id:
1068983
Local pid:
pubs:1068983
Language:
English
Format:
Print-Electronic

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