Letters in Drug Design & Discovery

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

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N-Aroylated Isatins: Antiglycation Activity

Author(s): Khalid Mohammed Khan, Uzma Rasool Mughal, Ambreen Khan, Farzana Naz, Shahnaz Perveen, M. Iqbal Choudhary.

Abstract:

A series of N-aroylated isatins 1-15 was synthesized and evaluated for their antiglycation activity. All compounds showed a varying degree of glycation inhibitory activity with IC50 values between 18.01 ± 0.05-693.7 ± 3.0 μM, when compared with the standard (aminoguanidine) having an IC50 = 268.7 ± 12.4 μM. Compound 1 was found to be the most active member of this series with an IC50 = 18.01 ± 0.05 μM. Compound 10 showed an IC50 = 72.5 ± 0.09 μM, whereas compound 7 has an IC50 = 80.18 ± 0.07 μM. Compounds 3, 9, and 13 showed IC50 values 170.2 ± 0.62, 117.91 ± 2.9, 171.3 ± 0.79 μM, respectively. Rest of the compounds along with parent isatin were found to be inactive. The structures of all the synthetic compounds were deduced by spectroscopic analysis.

Keywords: Isatin, N-Aroylation, Antiglycation, Lead molecules

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Article Details

VOLUME: 7
ISSUE: 3
Year: 2010
Page: [188 - 193]
Pages: 6
DOI: 10.2174/157018010790596597
Price: $58