Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors
| Autor: | Sekgota, Khethobole C, Majumder, Swarup, Isaacs, Michelle, Mnkandhla, Dumisani, Hoppe, Heinrich C, Khanye, Setshaba D, Kriel, Frederik H, Coates, Judy, Kaye, Perry T |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Druh dokumentu: | Článek |
| DOI: | 10.1016/j.bioorg.2017.09.015 |
| Popis: | publisher version A practicable six-step synthetic pathway has been developed to access a library of novel 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones using Morita-Baylis-Hillman methodology. These compounds and their 3-[(N-cycloalkylamino)methyl]-2-quinolone precursors have been screened as potential HIV-1 integrase (IN) inhibitors. A concomitant survey of their activity against HIV-1 protease and reverse-transcriptase reveals selective inhibition of HIV-1 IN. |
| Databáze: | Networked Digital Library of Theses & Dissertations |
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