DOI: 10.1039/d3md00242j ISSN: 2632-8682
Discovery of rigid biphenyl Plasmodium falciparum DHFR inhibitors using a fragment linking strategy
Marie Hoarau, Patpanat Sermmai, Thaveechai Varatthan, Ratthiya Thiabma, Tararat Jantra, Roonglawan Rattanajak, Danoo Vitsupakorn, Jarunee Vanichtanankul, Siriporn Saepua, Yongyuth Yuthavong, Chawanee Thongpanchang, Sumalee Kamchonwongpaisan- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
- Pharmacology
- Molecular Medicine
- Biochemistry
The screen of a fragment library identified hydrophobic fragments binding to drug resistant PfDHFR active site. Lead design using fragment-linking strategy yielded compounds with nM antimalarial activity, no cytotoxicity and drug-like properties.