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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

N-Aroylated Isatins: Antiglycation Activity

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

Volume 7, Issue 3, 2010

Page: [188 - 193] Pages: 6

DOI: 10.2174/157018010790596597

Price: $65

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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