Evaluation of novel N′-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors†,RSC Medicinal Chemistry

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Evaluation of novel N′-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-12-10 00:00:00 , DOI: 10.1039/c8md00328a
Omobolanle J Jesumoroti ₁ , Faridoon ₁ , Dumisani Mnkandhla _{2,

3} , Michelle Isaacs _{2,

3} , Heinrich C Hoppe _{2,

3} , Rosalyn Klein _{1,

3}

Affiliation

In an attempt to identify potential new agents that are active against HIV-1 IN, a series of novel coumarin-3-carbohydrazide derivatives were designed and synthesised. The toxicity profiles of these compounds showed that they were non-toxic to human cells and they exhibited promising anti-HIV-1 IN activities with IC₅₀ values in nM range. Also, an accompanying molecular modeling study showed that the compounds bind to the active pocket of the enzyme.

中文翻译：

评价新型 N'-(3-羟基苯甲酰基)-2-oxo-2H-chromene-3-carbohydrazide 衍生物作为潜在的 HIV-1 整合酶抑制剂†

为了确定对 HIV-1 IN 具有活性的潜在新药物，设计并合成了一系列新型香豆素-3-碳酰肼衍生物。这些化合物的毒性特征表明它们对人体细胞无毒，并且它们表现出有希望的抗 HIV-1 IN 活性，IC ₅₀值在 nM 范围内。此外，一项伴随的分子建模研究表明，这些化合物与酶的活性口袋结合。

更新日期：2018-12-10

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