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

• Main Authors: Marie Hoarau (Author), Jarunee Vanichtanankul (Author), Nitipol Srimongkolpithak (Author), Danoo Vitsupakorn (Author), Yongyuth Yuthavong (Author), Sumalee Kamchonwongpaisan (Author)
• Format: Book
• Published: Taylor & Francis Group, 2021-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...