Leung, Suet C. published the artcileIdentification, Design and Biological Evaluation of Heterocyclic Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2), Application of Ethyl 3-(4-iodophenyl)-3-oxopropanoate, the main research area is quinolone derivative preparation antimalarial Plasmodium NADH quinone oxidoreductase SAR.
Following a program undertaken to identify hit compounds against NADH:ubiquinone oxidoreductase (PfNDH2), a novel enzyme target within the malaria parasite Plasmodium falciparum, hit to lead optimization led to identification of CK-2-68, a mol. suitable for further development. To reduce ClogP and improve solubility of CK-2-68 incorporation of a variety of heterocycles, within the side chain of the quinolone core, was carried out, and this approach led to a lead compound SL-2-25 (I). I has IC50s in the nanomolar range vs. both the enzyme and whole cell P. falciparum (IC50 = 15 nM PfNDH2; IC50 = 54 nM (3D7 strain of P. falciparum)) with notable oral activity of ED50/ED90 of 1.87/4.72 mg/kg vs. Plasmodium berghei (NS Strain) in a murine model of malaria when formulated as a phosphate salt. Analogs in this series also demonstrate nanomolar activity against the bc1 complex of P. falciparum providing the potential added benefit of a dual mechanism of action. The potent oral activity of 2-pyridyl quinolones underlines the potential of this template for further lead optimization studies.
Journal of Medicinal Chemistry published new progress about Antimalarials. 63131-30-6 belongs to class iodides-buliding-blocks, name is Ethyl 3-(4-iodophenyl)-3-oxopropanoate, and the molecular formula is C11H11IO3, Application of Ethyl 3-(4-iodophenyl)-3-oxopropanoate.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com