Novel Pd(II) complexes of 1-N-substituted 3-phenyl-2-pyrazoline derivatives and evaluation of antiamoebic activity.
Cyclization of Mannich base with N(4)-substituted thiosemicarbazides by different aliphatic, aromatic and cyclic amines afforded a series of new 1-N-substituted cyclised pyrazoline analogues of thiosemicarbazones (PYZ-TSC) 1-10. Reaction of [Pd(DMSO)(2)Cl(2)] with pyrazoline derivatives led to new palladium(II) complexes [Pd(PYZ-TSC)Cl(2)] 1a-10a. The structures of all the compounds were characterized by spectroscopic methods. It was concluded that the pyrazoline thiosemicarbazone derivatives have two chelating arms, one attached at the 2-position of the pyrazole ring (that is, N donor) and other (S donor) linked to the thiosemicarbazone branch. The determination of antiamoebic activity of all the compounds was done using HM1:IMSS strain of Entamoeba histolytica, among all the complexes, 8a showed the most promising IC(50)=0.37 microM vs. IC(50)=1.81 microM of metronidazole, the reference drug. MTT assay showed that the compounds are non-toxic to human kidney epithelial cell line.
Husain
Kakul
K
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Abid
Mohammad
M
Azam
Amir
A
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004748:Entamoeba histolytica / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D010165:Palladium / Q000737:chemistry*; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
D000981:Antiprotozoal Agents; D011720:Pyrazoles; D010165:Palladium