Hybrid Inhibitors of Malarial Dihydrofolate Reductase with Dual Binding Modes That Can Forestall Resistance

[Image: see text] The S108N mutation of dihydrofolate reductase (DHFR) renders Plasmodium falciparum malaria parasites resistant to pyrimethamine through steric clash with the rigid side chain of the inhibitor. Inhibitors with flexible side chains can avoid this clash and retain effectiveness agains...

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Udgivet i:ACS Med Chem Lett
Main Authors: Tarnchompoo, Bongkoch, Chitnumsub, Penchit, Jaruwat, Aritsara, Shaw, Philip J., Vanichtanankul, Jarunee, Poen, Sinothai, Rattanajak, Roonglawan, Wongsombat, Chayaphat, Tonsomboon, Aunchalee, Decharuangsilp, Sasithorn, Anukunwithaya, Tosapol, Arwon, Uthai, Kamchonwongpaisan, Sumalee, Yuthavong, Yongyuth
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2018
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6295868/
https://ncbi.nlm.nih.gov/pubmed/30613332
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00389
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