Synthesis and antileishmanial activity of novel pyridinium-hydrazone derivatives

A series of substituted phenylethylidenehydrazinylpyridinium derivatives bearing methyl, ethyl, propyl, and propylphenyl groups on the pyridinium nitrogen were synthesized and evaluated for in vitro antileishmanial activity against Leishmania tropica by using the microdilution method. Among the test...

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Bibliographic Details
Published in:Journal of enzyme inhibition and medicinal chemistry 2013-10, Vol.28 (5), p.960-967
Main Authors: Alptuzun, Vildan, Cakiroglu, Gokcer, Limoncu, M. Emin, Erac, Bayri, Hosgor-Limoncu, Mine, Erciyas, Ercin
Format: Article
Language:English
Subjects:
antileishmanial activity
Antiprotozoal Agents - chemical synthesis
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
Dose-Response Relationship, Drug
hydrazone
Hydrazones - chemical synthesis
Hydrazones - chemistry
Hydrazones - pharmacology
Leishmania tropica - drug effects
Molecular Structure
Parasitic Sensitivity Tests
promastigote
Pyridinium Compounds - chemical synthesis
Pyridinium Compounds - chemistry
Pyridinium Compounds - pharmacology
Pyridinium salts
Structure-Activity Relationship
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Summary:A series of substituted phenylethylidenehydrazinylpyridinium derivatives bearing methyl, ethyl, propyl, and propylphenyl groups on the pyridinium nitrogen were synthesized and evaluated for in vitro antileishmanial activity against Leishmania tropica by using the microdilution method. Among the tested compounds, 3d, 5c, 3b, and 3c were found to be the most active derivatives against the promastigotes of L. tropica (IC50 values are 6.90, 9.92, 11.69 and 12.03 µM, respectively) and to be more active than reference drug meglumine antimonaite (glucantime) (IC50 value: 20.49 µM). The derivatives investigated in this study may have the potential to be lead compound against leishmanial infection.
ISSN:1475-6366
1475-6374
DOI:10.3109/14756366.2012.697058