Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro

Author(s): Rui-Ge Yang, Liu-Meng Yang, Ya-Zhen Ke, Ning Huang, Rui Zhang, Yong-Tang Zheng, Hui Xu.

Abstract:

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

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Article Details

VOLUME: 9
ISSUE: 4
Year: 2012
Page: [415 - 420]
Pages: 6
DOI: 10.2174/157018012799859936
Price: $58