Synthesis and antileishmanial activity of novel pyridinium-hydrazone derivatives


Alptuzun V. , Cakiroglu G., Limoncu M. E. , Erac B. , Hosgor-Limoncu M., Erciyas E.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.28, ss.960-967, 2013 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 28 Konu: 5
  • Basım Tarihi: 2013
  • Doi Numarası: 10.3109/14756366.2012.697058
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Sayfa Sayıları: ss.960-967

Özet

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 mu M, respectively) and to be more active than reference drug meglumine antimonaite (glucantime) (IC50 value: 20.49 mu M). The derivatives investigated in this study may have the potential to be lead compound against leishmanial infection.