1076088-50-0

WRR-483, an analogue of K-11777, is a potent and selective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777. WRR-483 demonstrates good potency against cruzain with sensitivity to pH conditions and high efficacy in the cell culture assay. Furthermore, WRR-483 also eradicates parasite infection in a mouse model of acute Chagas' disease. WRR-483 binds covalently to the active site cysteine of the protease in a similar manner as other vinyl sulfone-based inhibitors. WRR-483 has potential to be developed as a treatment for Chagas' disease.

WRR-483 是 K11777 的类似物，是克鲁兹蛋白酶（cruzain）的抑制剂，用于细胞培养中对克氏锥虫的增殖抑制。WRR-483 在急性恰加斯病小鼠模型中能根除寄生虫感染。WRR-483 是不可逆的半胱氨酸蛋白酶抑制剂，对克鲁兹蛋白酶和 T. cruzi 感染显示出 pH 依赖的高亲和力和有效的杀锥虫活性，有望抑制恰加斯病。