Synthesis and antileishmanial activity of novel pyridinium-hydrazone derivatives
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Date
2013
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Abstract
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. © 2013 Informa UK, Ltd.
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Antiprotozoal Agents , Dose-Response Relationship, Drug , Hydrazones , Leishmania tropica , Molecular Structure , Parasitic Sensitivity Tests , Pyridinium Compounds , Structure-Activity Relationship , 1 ethyl 4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] pyridinium bromide , 1 ethyl 4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] pyridinium bromide , 1 ethyl 4 [2 (1 phenylethylidene)hydrazinyl]pyridinium bromide , 1 methyl 4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] pyridinium iodide , 1 methyl 4 [2 (1 phenylethylidene)hydrazinyl]pyridinium iodide , 4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 (3 phenylpropyl)pyridinium bromide , 4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 ethylpyridinium bromide , 4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 methylpyridinium iodide , 4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 propylpyridinium bromide , 4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] 1 (3 phenylpropyl)pyridinium bromide , 4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] 1 methylpyridinium iodide , 4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] 1 propylpyridinium bromide , 4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] 1 (3 phenylpropyl)pyridinium bromide , 4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] 1 propylpyridinium bromide , 4 [2 (1 phenylethylidene)hydrazinyl] 1 (3 phenylpropyl) pyridinium bromide , 4 [2 (1 phenylethylidene)hydrazinyl] 1 propyl pyridinium bromide , antileishmanial agent , dimethyl sulfoxide , hydrazone derivative , meglumine antimonate , phenylethylidenehydrazinylpyridine , pyridine derivative , pyridinium derivative , unclassified drug , antiprotozoal activity , article , bacterial growth , bacterial infection , biological activity , concentration response , controlled study , drug synthesis , heteronuclear nuclear magnetic resonance , IC 50 , in vitro study , Leishmania tropica , nonhuman , priority journal , promastigote , skin leishmaniasis