Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors
设计和合成含双酰胺和酰肼的丙二酸衍生物作为潜在的 HIV-1 整合酶抑制剂
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作者:Mario Sechi, Ugo Azzena, Maria Paola Delussu, Roberto Dallocchio, Alessandro Dessì, Alessia Cosseddu, Nicolino Pala, Nouri Neamati
| 期刊: | Molecules | 影响因子: | 4.200 |
| 时间: | 2008 | 起止号: | 2008 Oct 1;13(10):2442-61. |
| doi: | 10.3390/molecules13102442 | 研究方向: | 免疫 |
| 疾病类型: | 艾滋病 | |
Abstract
HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site.
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