Syntheses, characterization and in vitro antiamoebic activity of new Pd(II) complexes with 1-N-substituted thiocarbamoyl-3,5-diphenyl-2-pyrazoline derivatives.
Reaction of neutral NS bidentate ligands, 1-N-substituted thiocarbamoyl-3,5-diphenyl-2-pyrazolines, isolated by cyclization of chalcone with N-4-substituted thiosemicarbazide of aromatic amines (1-8), with [Pd(DMSO)(2)Cl(2)] (DMSO=dimethylsulfoxide) leads to the formation of new complexes of the type [Pd(L)Cl(2)] (1a-8a). The structures of the compounds were elucidated by UV, IR, (1)H NMR, (13)C NMR and ESI-MS spectral data and thermogravimetric analysis and their purities were confirmed by elemental analyses. The antiamoebic activity of these complexes was evaluated by microdilution method against HM1:IMSS strain of Entameoba histolytica and the results were compared with the standard drug, metronidazole. Generally palladium complexes showed better activity than their corresponding ligands. Compound 3a showed better IC(50)=0.05 microM as compared to metronidazole IC(50)=1.82 microM.
Budakoti
Asha
A
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Abid
Mohammad
M
Azam
Amir
A
D000563:Amebicides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D004748:Entamoeba histolytica / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010165:Palladium / Q000737:chemistry*; D021261:Parasitic Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D021241:Spectrometry, Mass, Electrospray Ionization; D013890:Thiourea / Q000737:chemistry*
D000563:Amebicides; D009942:Organometallic Compounds; D011720:Pyrazoles; D010165:Palladium; D013890:Thiourea