Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro
Rui-Ge Yang, Liu-Meng Yang, Ya-Zhen Ke, Ning Huang, Rui Zhang, Yong-Tang Zheng, Hui Xu.
Twenty-one 2-(N-arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones (4a-u) were synthesized and evaluated
as HIV-1 inhibitors in vitro. Among all compounds, compounds 4n and 4p displayed the potent anti-HIV-1 activities with
EC50 values of 3.48 and 8.61 μg/mL, and TI values of 34.08 and > 23.22, respectively. It demonstrated that, to a series of
2-(N-arylsulfonyl-6-methylindol-3-yl)-3-aryl-1,3-thiazolidin-4-one derivatives, introduction of R2 as 4-Cl and R3 as H or
3-Cl could afford the more promising and potent compounds.
Keywords: 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1, 3-thiazolidin-4-ones, Acquired immunodeficiency syndrome, Human
immunodeficiency virus-1, AIDS
Rights & PermissionsPrintExport