具有抗 HIV 活性的喹诺酮-3-羧酸的结构修饰。
Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity.
机构信息
Department of Chemistry, Fudan University, Shanghai 200433, PR China.
出版信息
Bioorg Med Chem. 2011 Aug 15;19(16):5039-45. doi: 10.1016/j.bmc.2011.06.020. Epub 2011 Jul 15.
A series of new quinolone-3-carboxylic acids featuring a hydroxyl group at C-5 position were synthesized and evaluated for their in vitro activity against HIV in C8166 cell culture. All the compounds showed anti-HIV-1 activity with low micromolar to submicromolar EC(50) values. The most active compound 2k exhibited activity against wild-type HIV-1 with an EC(50) value of 0.13 μΜ. Preliminary structure-activity relationship of the newly synthesized quinolone analogues was also investigated. Further docking study revealed that the anti-HIV activity of these compounds might involve a two-metal chelating mechanism.
一系列在 C-5 位带有羟基的新型喹诺酮-3-羧酸被合成出来，并在 C8166 细胞培养中评估其对 HIV 的体外活性。所有化合物均表现出抗 HIV-1 活性，EC(50) 值为低微摩尔至亚微摩尔。最活性化合物 2k 对野生型 HIV-1 的活性 EC(50) 值为 0.13 μΜ。还对新合成的喹诺酮类似物的初步构效关系进行了研究。进一步的对接研究表明，这些化合物的抗 HIV 活性可能涉及双金属螯合机制。
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