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UCT943, a next generation plasmodium falciparum PI4K inhibitor preclinical candidate for the treatment of malaria

Abstract:

The 2-aminopyridine MMV048 was the first drug candidate inhibiting Plasmodium phosphatidylinositol 4-kinase (PI4K), a novel drug target for malaria, to enter clinical development. In an effort to identify the next generation of PI4K inhibitors, the series was optimized to improve properties such as solubility and antiplasmodial potency across the parasite lifecycle, leading to the 2-aminopyrazine UCT943. The compound displayed higher asexual blood stage, transmission-blocking, and liver stage...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1128/aac.00012-18

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ORCID:
0000-0003-2397-3174
Lawrence, N More by this author
Njoroge, M More by this author
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Technology Innovation Agency More from this funder
Strategic Health Innovation Partnerships More from this funder
South African Medical Research Council More from this funder
Publisher:
American Society for Microbiology Publisher's website
Journal:
Antimicrobial Agents and Chemotherapy Journal website
Volume:
62
Issue:
9
Pages:
e00012-18
Publication date:
2018-08-27
Acceptance date:
2018-06-25
DOI:
EISSN:
1098-6596
ISSN:
0066-4804
Pubs id:
pubs:859868
URN:
uri:14edbcdb-ccd5-434f-ac7a-4c93ad57a0d7
UUID:
uuid:14edbcdb-ccd5-434f-ac7a-4c93ad57a0d7
Local pid:
pubs:859868
Language:
English

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