Sekgota Khethobole C, Majumder Swarup, Isaacs Michelle, Mnkandhla Dumisani, Hoppe Heinrich C, Khanye Setshaba D, Kriel Frederik H, Coates Judy, Kaye Perry T
Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Bioorg Chem. 2017 Dec;75:310-316. doi: 10.1016/j.bioorg.2017.09.015. Epub 2017 Sep 22.
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.
已开发出一种可行的六步合成途径，利用森田-贝利斯-希尔曼方法获得一系列新型3-[(N-环烷基苯甲酰胺基)甲基]-2-喹诺酮类化合物。这些化合物及其3-[(N-环烷基氨基)甲基]-2-喹诺酮前体已被筛选为潜在的HIV-1整合酶（IN）抑制剂。同时对它们针对HIV-1蛋白酶和逆转录酶的活性进行的研究表明，它们对HIV-1整合酶具有选择性抑制作用。
