二脱氨-1,3-二氧代六氢吡嗪，是一种有效的抗疟药物，在体外和体内均有活性。
Diatretol, an α, α'-dioxo-diketopiperazine, is a potent in vitro and in vivo antimalarial.
机构信息
Ōmura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
出版信息
J Antibiot (Tokyo). 2021 Apr;74(4):266-268. doi: 10.1038/s41429-020-00390-2. Epub 2021 Jan 14.
A fungal metabolite, diatretol, has shown to be a promising antimalarial agent. Diatretol displayed potent in vitro antiparasitic activity against the Plasmodium falciparum K1 strain, with an IC value of 378 ng ml, as well as in vivo efficacy in a Plasmodium berghei-infected mice model, with ca. 50% inhibition at 30 mg/kg (p.o.).
真菌代谢产物 diatretol 已被证明是一种很有前途的抗疟药物。Diatretol 对恶性疟原虫 K1 株表现出很强的体外抗寄生虫活性，IC 值为 378ng/ml，在感染疟原虫伯氏疟原虫的小鼠模型中也具有体内疗效，在 30mg/kg（po）时约有 50%的抑制作用。
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