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Letters in Drug Design & Discovery

Editor-in-Chief

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

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 and Fatima Z. Basha

Volume 12, Issue 7, 2015

Page: [597 - 606] Pages: 10

DOI: 10.2174/1570180812999150225111959

Price: $65

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.

Graphical Abstract


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