Evaluation of novel N'-(3-hydroxybenzoyl)-2-oxo-2 H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors
新型 N'-(3-羟基苯甲酰)-2-氧代-2 H-色烯-3-碳酰肼衍生物作为潜在 HIV-1 整合酶抑制剂的评价
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作者:Omobolanle J Jesumoroti, Faridoon, Dumisani Mnkandhla, Michelle Isaacs, Heinrich C Hoppe, Rosalyn Klein
| 期刊: | Medchemcomm | 影响因子: | |
| 时间: | 2018 | 起止号: | 2018 Dec 10;10(1):80-88. |
| doi: | 10.1039/c8md00328a | 研究方向: | 免疫 |
| 疾病类型: | 艾滋病 | |
Abstract
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.
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