Inhibitors of Multiple Mutants of Plasmodium f alciparum Dihydrofolate Reductase and Their Antimalarial Activities

S Kamchonwongpaisan, R Quarrell…

文献索引：Yuthavong, Yongyuth; Vilaivan, Tirayut; Chareonsethakul, Netnapa; Kamchonwongpaisan, Sumalee; Sirawaraporn, Worachart; Quarrell, Rachel; Lowe, Gordon Journal of Medicinal Chemistry, 2000 , vol. 43, # 14 p. 2738 - 2744

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被引用次数: 82

摘要

Novel analogues of pyrimethamine (Pyr) and cycloguanil (Cyc) have been synthesized and tested as inhibitors of Plasmodium falciparum dihydrofolate reductase carrying triple (N51I+ C59R+ S108N, C59R+ S108N+ I164L) and quadruple (N51I+ C59R+ S108N+ I164L) mutations responsible for antifolate resistance. The inhibitors were designed to avoid steric clash of the p-Cl group of the inhibitors with the side chain of Asn108, augmented by ...