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Tetrahydrofuran tetrahydropyran triazoles and related heterocyclic derivatives as HIV protease inhibitors

机译:四氢呋喃四氢吡喃三唑和相关的杂环衍生物作为HIV蛋白酶抑制剂

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摘要

HIV/AIDS remains a formidable disease with millions of individuals inflicted worldwide. Although treatment regimens have improved considerably, drug resistance brought on by viral mutation continues to erode their effectiveness. Intense research efforts are currently underway in search of new and improved therapies. This review is concerned with the design of novel HIV-1 protease inhibitors that incorporate heterocyclic scaffolds and which have been reported within the recent literature (2005–2010). Various examples in this review showcase the essential role heterocycles play as scaffolds and bioisosteres in HIV-1 protease inhibitor drug development. This review will hopefully stimulate the widespread application of these heterocycles in the design of other therapeutic agents.
机译:艾滋病毒/艾滋病仍然是一种可怕的疾病,全世界有数百万人受到感染。尽管治疗方案已大大改善,但病毒突变引起的耐药性继续削弱其有效性。为了寻找新的和改进的疗法,目前正在进行大量的研究工作。这篇评论与新型HIV-1蛋白酶抑制剂的设计有关,该抑制剂结合了杂环支架,并且在最近的文献(2005-2010)中已有报道。这篇综述中的各种例子展示了杂环在HIV-1蛋白酶抑制剂药物开发中作为支架和生物等排物发挥的重要作用。这篇综述有望刺激这些杂环在其他治疗剂设计中的广泛应用。

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