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.
Letters in Drug Design & Discovery
Title:Synthesis and In vitro Evaluation of Dibenzoazepine Triazole Derivatives: A Novel Class of Antileishmanial Agents
Volume: 12 Issue: 7
Author(s): Maria Aqeel Khan, Aliyan Saleem, Nida Ghouri, Abdul Hameed, M. Iqbal Choudhary and Fatima Z. Basha
Affiliation:
Keywords: Dibenzoazepine, iminostilbene, antileishmanial, click chemistry, immunomodulatory, triazoles.
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.
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Aqeel Khan Maria, Saleem Aliyan, Ghouri Nida, Hameed Abdul, Choudhary Iqbal M. and Basha Z. Fatima, Synthesis and In vitro Evaluation of Dibenzoazepine Triazole Derivatives: A Novel Class of Antileishmanial Agents, Letters in Drug Design & Discovery 2015; 12 (7) . https://dx.doi.org/10.2174/1570180812999150225111959
DOI https://dx.doi.org/10.2174/1570180812999150225111959 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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