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Review Article

硝基化合物作为锥虫病和利什曼病的药物的当前和未来前景

卷 26, 期 23, 2019

页: [4454 - 4475] 页: 22

弟呕挨: 10.2174/0929867325666180426164352

价格: $65

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摘要

近年来，对用于治疗感染性疾病的硝基杂环药物的兴趣重新出现。 在这里，我们回顾一下单环和双环硝基杂环化合物作为内脏利什曼病，恰加斯氏病和人类非洲锥虫病的现有或潜在新疗法的现状。 单环（硝呋替莫斯，苯并咪唑和非线虫唑）和双环（前香豆素前体（PA-824）和德拉曼尼啶（OPC-67683））硝基化合物都是前药，需要酶促活化才能发挥其寄生虫毒性。 讨论了目前对激活中涉及的硝基还原酶的理解以及寄生虫产生抗性的可能机制，并描述了药物与实验化合物的药代动力学/药效行为以及化学结构-活性关系。

关键词: 非洲人锥虫病，恰加斯氏病，内脏利什曼病，尼呋替莫斯，苯硝唑，非辛达唑，前驱体，地拉曼尼，硝基药物。

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