Drug Development
Inhibitors of multiresistant P. falciparum DHFR synthesized
Published in Anti-Infectives Week, March 15th, 2004
According to recent research from Thailand, "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 additional mutations of the resistant mutants," explained S. Kamchonwongpaisan and coauthors at the National...
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Source: Anti-Infectives Week (2004-03-15)
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