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基于二基基和异芳基的烯胺基来应对HIV-1LEDGF/p75-依赖于IN活动的HIV-1LEDGF/p75-依赖于IN活动的HIV-1

Graziella Tocco¹, Serena Canton¹, Antonio Laus¹

¹Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, 09042 Monserrato, Italy.

Molecules (Basel, Switzerland)

|September 28, 2023

概括

新型诺皮里米丁衍生物显示出作为人类免疫缺陷病毒1型整合酶 (HIV-1 IN) 选择性抑制剂的前景. 这些化合物可能通过作为全抑制剂来提供针对耐药HIV菌株的新策略.

科学领域:

药用化学医学化学
病毒学病毒学
药物发现药物发现药物发现

背景情况:

人类免疫缺陷病毒 (HIV) 仍然是一个重大的全球健康问题.
艾滋病毒-1整合酶 (IN) 是药物开发的关键病毒标,因为它不在人体细胞中.
耐药性HIV菌株的出现需要开发新型全抑制剂.

研究的目的:

为了研究基于二基基的新型烯胺衍生物对它们的人类免疫缺陷病毒1型整合酶 (HIV-1 IN) 抑制活性.
探索结构-活性关系,重点关注基组在基部分上的位置.
为了确定HIV-1 IN的选择性和强大的全抑制剂.

主要方法:

合成和评估新型的二胺衍生物.
对依赖LEDGF/p75的HIV-1 IN抑制活性进行评估.
结构-活性关系分析和细胞毒性评估.
进行紫外线光谱实验以阐明作用机制.

主要成果:

观察到基组在环上的位置与IN抑制活性之间的相关性.
化合物21-23,25和26表现出增强的IN抑制活性.
化合物25成为IN最有选择性的抑制剂.
紫外线数据表明一种全性作用机制,与典型的Mg2+化INSTIs不同.

结论:

新的诺皮里米丁衍生物是HIV-1 IN的有效抑制剂.
环上的替代模式显著影响抑制活性和选择性.
这些化合物代表了开发新的抗艾滋病毒全抑制剂的有希望的领先候选人.

关键词:

艾滋病毒-1整合酶 (IN)LEDGF/p75依赖的IN活动类固醇抑制剂类固醇抑制剂类固醇抑制剂这种类型的 thienopyrimidinones.

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