Bristol Myers Squibb, San Diego, California 92121, United States.
Zoetis, Kalamazoo, Michigan 49001, United States.
J Med Chem. 2022 Aug 25;65(16):11388-11403. doi: 10.1021/acs.jmedchem.2c00960. Epub 2022 Aug 16.
Filarial diseases, including lymphatic filariasis and onchocerciasis, are considered among the most devastating of all tropical diseases, affecting about 145 million people worldwide. Efforts to control and eliminate onchocerciasis are impeded by a lack of effective treatments that target the adult filarial stage. Herein, we describe the discovery of a series of substituted di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as novel macrofilaricides for the treatment of human filarial infections.
丝虫病,包括淋巴丝虫病和盘尾丝虫病,被认为是所有热带病中最具破坏性的疾病之一,影响全球约 1.45 亿人。由于缺乏针对成虫阶段的有效治疗方法,控制和消除盘尾丝虫病的工作受到阻碍。在此,我们描述了一系列取代的二(吡啶-2-基)-1,2,4-噻二唑-5-胺作为新型的大环丝虫药物的发现,用于治疗人类丝虫感染。