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Article

Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.

Journal of medicinal chemistry - 29 Jan 2004

Kamchonwongpaisan Sumalee, Quarrell Rachel, Charoensetakul Netnapa, Ponsinet Rachel, Vilaivan Tirayut, Vanichtanankul Jarunee, Tarnchompoo Bongkoch, Sirawaraporn Worachart, Lowe Gordon, Yuthavong Yongyuth

Abstract excerpt

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,...

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PMID: 14736247
DOI: 10.1021/jm030165t

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