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 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.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University , Bornova, Izmir , Turkey.
Vildan
V
Alptuzun
Gokcer
G
Cakiroglu
M Emin
ME
Limoncu
Bayri
B
Erac
Mine
M
Hosgor-Limoncu
Ercin
E
Erciyas
D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007895:Leishmania tropica / Q000187:drug effects*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011726:Pyridinium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D006835:Hydrazones; D011726:Pyridinium Compounds