Discovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening

Discovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening

In various malaria-endemic regions, the appearance of resistance has precluded the use of pyrimidine-based antifolate drugs. Here, a three-step fragment screening was used to identify new non-pyrimidine Plasmodium falciparum dihydrofolate reductase (PfDHFR) inhibitors. Starting from a 1163-fragment...

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Bibliographic Details
Main Authors: Marie Hoarau, Jarunee Vanichtanankul, Nitipol Srimongkolpithak, Danoo Vitsupakorn, Yongyuth Yuthavong, Sumalee Kamchonwongpaisan
Format: Article
Language:English
Published: Taylor & Francis Group 2021-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
malaria
plasmodium falciparum
fragment-based screening
dihydrofolate reductase
small molecule inhibitors
Online Access:http://dx.doi.org/10.1080/14756366.2020.1854244

Internet

http://dx.doi.org/10.1080/14756366.2020.1854244

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