Cheviet, Thomas; Wein, Sharon; Bourchenin, Gabriel; Lagacherie, Manon; Perigaud, Christian; Cerdan, Rachel; Peyrottes, Suzanne published their research in Journal of Medicinal Chemistry on August 13 ,2020. The article was titled 《β-Hydroxy- and β-Aminophosphonate Acyclonucleosides as Potent Inhibitors of Plasmodium falciparum Growth》.Safety of (R)-Oxiran-2-ylmethanol The article contains the following contents:
Malaria is an infectious disease caused by a parasite of the genus Plasmodium, and the emergence of parasites resistant to all current antimalarial drugs highlights the urgency of having new classes of mols. We developed an effective method for the synthesis of a series of β-modified acyclonucleoside phosphonate (ANP) derivatives, using com. available and inexpensive materials (i.e., aspartic acid and purine heterocycles). Their biol. evaluation in cell culture experiments and SAR revealed that the compounds’ effectiveness depends on the presence of a hydroxyl group, the chain length (four carbons), and the nature of the nucleobase (guanine). The most active derivative I inhibits the growth of Plasmodium falciparum in vitro in the nanomolar range (IC50 = 74 nM) with high selectivity index (SI > 1350). This compound also showed remarkable in vivo activity in P. berghei-infected mice (ED50 ~0.5 mg/kg) when administered by the i.p. route and is, although less efficient, still active via the oral route. It is the first ANP derivative with such potent antimalarial activity and therefore has considerable potential for development as a new antimalarial drug. The experimental part of the paper was very detailed, including the reaction process of (R)-Oxiran-2-ylmethanol(cas: 57044-25-4Safety of (R)-Oxiran-2-ylmethanol)
(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Safety of (R)-Oxiran-2-ylmethanol
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