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- W2892262777 abstract "Severe malaria due to Plasmodium falciparum remains a significant global health threat. DXR, the second enzyme in the MEP pathway, plays an important role to synthesize building blocks for isoprenoids. This enzyme is a promising drug target for malaria due to its essentiality as well as its absence in humans. In this study, we designed and synthesized a series of α,β-unsaturated analogues of fosmidomycin, a natural product that inhibits DXR in P. falciparum. All compounds were evaluated as inhibitors of P. falciparum. The most promising compound, 18a, displays on-target, potent inhibition against the growth of P. falciparum (IC50 = 13 nM) without significant inhibition of HepG2 cells (IC50 > 50 μM). 18a was also tested in a luciferase-based Plasmodium berghei mouse model of malaria and showed exceptional in vivo efficacy. Together, the data support MEPicide 18a as a novel, potent, and promising drug candidate for the treatment of malaria." @default.
- W2892262777 created "2018-09-27" @default.
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- W2892262777 date "2018-09-07" @default.
- W2892262777 modified "2023-10-16" @default.
- W2892262777 title "MEPicides: α,β-Unsaturated Fosmidomycin Analogues as DXR Inhibitors against Malaria" @default.
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- W2892262777 doi "https://doi.org/10.1021/acs.jmedchem.8b01026" @default.
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