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Review Article

含三唑杂环化合物：抗锥虫克鲁齐药物开发中的特权支架

卷 23, 期 1, 2022

发表于: 12 April, 2021

页: [33 - 59] 页: 27

弟呕挨: 10.2174/1389450122666210412125643

价格: $65

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摘要

背景：南美锥虫病是一种由原生动物寄生虫克氏锥虫引起的潜在危及生命的疾病，并通过受感染的吸血三角螟虫的排泄物传播给人类。根据世界卫生组织的数据，全世界有 6 到 700 万人感染了 T. cruzi，主要在拉丁美洲，每年有超过 10000 人死亡。 研究目的：本研究旨在提供关于含三唑杂环在开发抗恰加斯病药物中重要性的综合文献信息。 方法：在 2020 年 12 月之前使用各种电子数据库（包括 SciFinder、PubMed（国家医学图书馆）、Science Direct、Wiley、ACS（美国化学学会）、SciELO（在线科学电子图书馆）、谷歌）获取了包含的信息，没有日期限制Scholar、Springer、Scopus 和 Web of Science。 结果：在体外研究中，100 多种含三唑杂环化合物被预测为可对抗导致美国锥虫病的病原体的活性化合物。然而，关于它们在动物模型中的体内活性和它们在人类中的临床研究知之甚少。此外，这些生物活性化合物的药代动力学研究仍在进行中。尽管大多数这些分子具有多种作用机制，但所涉及的确切机制仍然存在争议。因此，体内实验，其次是药代动力学，以及最活跃的化合物的作用机制，应该是未来研究的主题。结论：总而言之，最近的研究证明了含三唑杂环化合物在寻找潜在候选药物开发抗恰加斯病的重要性。尽管如此，新催化剂的使用和化学转化有望为合成未开发的三唑衍生物提供途径，从而开发出具有新性质和杀锥虫活性的含三唑化合物。

关键词: 三唑类、美洲锥虫病、原生动物寄生虫、合成、药物发现、被忽视的疾病。

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