Article
Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
European journal of medicinal chemistry - 1 Jun 2020
Kamchonwongpaisan Sumalee, Charoensetakul Netnapa, Srisuwannaket Choladda, Taweechai Supannee, Rattanajak Roonglawan, Vanichtanankul Jarunee, Vitsupakorn Danoo, Arwon Uthai, Thongpanchang Chawanee, Tarnchompoo Bongkoch, Vilaivan Tirayut, Yuthavong Yongyuth
Abstract excerpt
A series of flexible diaminodihydrotriazines or cycloguanil (Cyc) analogues are developed and shown to inhibit P. falciparum dihydrofolate reductase (PfDHFR) of the wild type or those carrying either single (S108N), double (C59R + S108N and A16V + S108T), triple (N51I + C59R + S108N and C59R + S108N + I164L) or quadruple (N51I + C59R + S108N + I164L) mutations, responsible for antifolate resistance. The...
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