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Article

Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.

Journal of medicinal chemistry - 26 Jun 2014

Deng Xiaoyi, Kokkonda Sreekanth, El Mazouni Farah, White John, Burrows Jeremy N, Kaminsky Werner, Charman Susan A, Matthews David, Rathod Pradipsinh K, Phillips Margaret A

Abstract excerpt

Malaria is one of the most serious global infectious diseases. The pyrimidine biosynthetic enzyme Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) is an important target for antimalarial chemotherapy. We describe a detailed analysis of protein-ligand interactions between DHODH and a triazolopyrimidine-based inhibitor series to explore the effects of fluorine on affinity and species selectivity. We...

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Identifiers

PMID: 24801997
DOI: 10.1021/jm500481t
PMCID: PMC4079327

Genes

DHODH

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