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J Enzyme Inhib Med Chem ; 28(5): 960-7, 2013 Oct.
Article in English | MEDLINE | ID: mdl-22803671

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.


Subject(s)
Antiprotozoal Agents/pharmacology , Hydrazones/pharmacology , Leishmania tropica/drug effects , Pyridinium Compounds/pharmacology , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Dose-Response Relationship, Drug , Hydrazones/chemical synthesis , Hydrazones/chemistry , Molecular Structure , Parasitic Sensitivity Tests , Pyridinium Compounds/chemical synthesis , Pyridinium Compounds/chemistry , Structure-Activity Relationship
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