Alptuzun V.Cakiroglu G.Limoncu M.E.Erac B.Hosgor-Limoncu M.Erciyas E.2024-07-222024-07-22201314756374http://akademikarsiv.cbu.edu.tr:4000/handle/123456789/17266A 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.EnglishAll Open Access; Bronze Open AccessAntiprotozoal AgentsDose-Response Relationship, DrugHydrazonesLeishmania tropicaMolecular StructureParasitic Sensitivity TestsPyridinium CompoundsStructure-Activity Relationship1 ethyl 4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] pyridinium bromide1 ethyl 4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] pyridinium bromide1 ethyl 4 [2 (1 phenylethylidene)hydrazinyl]pyridinium bromide1 methyl 4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] pyridinium iodide1 methyl 4 [2 (1 phenylethylidene)hydrazinyl]pyridinium iodide4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 (3 phenylpropyl)pyridinium bromide4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 ethylpyridinium bromide4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 methylpyridinium iodide4 [2 (1 [4 chlorophenyl]ethylidene)hydrazinyl] 1 propylpyridinium bromide4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] 1 (3 phenylpropyl)pyridinium bromide4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] 1 methylpyridinium iodide4 [2 (1 [4 methoxylphenyl]ethylidene)hydrazinyl] 1 propylpyridinium bromide4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] 1 (3 phenylpropyl)pyridinium bromide4 [2 (1 [4 methylphenyl]ethylidene)hydrazinyl] 1 propylpyridinium bromide4 [2 (1 phenylethylidene)hydrazinyl] 1 (3 phenylpropyl) pyridinium bromide4 [2 (1 phenylethylidene)hydrazinyl] 1 propyl pyridinium bromideantileishmanial agentdimethyl sulfoxidehydrazone derivativemeglumine antimonatephenylethylidenehydrazinylpyridinepyridine derivativepyridinium derivativeunclassified drugantiprotozoal activityarticlebacterial growthbacterial infectionbiological activityconcentration responsecontrolled studydrug synthesisheteronuclear nuclear magnetic resonanceIC 50in vitro studyLeishmania tropicanonhumanpriority journalpromastigoteskin leishmaniasisArticle10.3109/14756366.2012.697058