Letters in Drug Design & Discovery

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

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Synthesis and In vitro Evaluation of Dibenzoazepine Triazole Derivatives: A Novel Class of Antileishmanial Agents

Author(s): Maria Aqeel Khan, Aliyan Saleem, Nida Ghouri, Abdul Hameed, M. Iqbal Choudhary, Fatima Z. Basha.

Graphical Abstract:


Abstract:

In the present study, a series of dibenzoazepine triazole derivatives (24-39) were synthesized and evaluated for their in vitro bioactivities including antiglycation, antibacterial, DPPH radical scavenging, urease inhibition, antileishmanial and immunomodulatory activities. The compounds were found to be moderately active only against leishmania. Within this series, compound 26 was found to be the most active antileishaminals with IC50 value 37.4 ± 0.4 µM. Structure-activity relationships for this novel class are discussed.

Keywords: Dibenzoazepine, iminostilbene, antileishmanial, click chemistry, immunomodulatory, triazoles.

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Article Details

VOLUME: 12
ISSUE: 7
Year: 2015
Page: [597 - 606]
Pages: 10
DOI: 10.2174/1570180812999150225111959
Price: $58