Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3534-6. doi: 10.1016/j.bmcl.2010.04.132. Epub 2010 May 18.
In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC(50) values of 0.36 and 0.13 microg/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs.
在我们旨在发现和开发具有优异抗人类免疫缺陷病毒 1 型 (HIV-1) 活性的化合物的计划中，合成了 21N-芳基磺酰基-3-乙酰基吲哚类似物 (2a-u)，并初步评估了它们作为 HIV-1 抑制剂的体外活性。在所有类似物中，有几个化合物表现出显著的抗 HIV-1 活性，特别是 N- 苯基磺酰基-3-乙酰基-6-甲基吲哚 (2j) 和 N-(p-乙基)苯基磺酰基-3-乙酰基-6-甲基吲哚 (2n) 表现出最强的抗 HIV-1 活性，EC(50) 值分别为 0.36 和 0.13 μg/mL，TI 值分别为 >555.55 和 791.85。这表明在 N-芳基磺酰基-6-甲基吲哚的 3-位引入乙酰基通常可以得到更有效的类似物。
