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Synthesis and evaluation of substituted 4-arylimino-3-hydroxybutanoic acids as potential HIV-1 integrase inhibitors |
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| Authors: | Dumisani Mnkandhla Michelle Isaacs Heinrich C Hoppe Perry T Kaye |
| Institution: | 1. Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa;2. Department of Biochemistry and Microbiolgy, Rhodes University, Grahamstown 6140, South Africa;3. Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa |
| Abstract: | A series of readily accessible 4-arylimino-3-hydroxybutanoic acids have been prepared and evaluated as potential HIV-1 Integrase inhibitors. None of the ligands exhibited significant toxicity against human embryonic kidney (HEK 293) cells, while five of them showed activity against HIV-1 integrase – the most active (6c) with an IC50 value of 3.5?μM. In silico docking studies indicate the capacity of ligand 6c to interact with several amino acid residues and the two Mg2+ cations in the HIV-1 integrase receptor cavity. |
| Keywords: | HIV-1 integrase inhibitors Synthesis 4-Arylimino-3-hydroxybutanoic acids |
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