title: Palladium(II) complexes of OS donor N-(di(butyl/phenyl)carbamothioyl)benzamide and their antiamoebic activity.
abstract: Two promising palladium(II) compounds of general formula, cis-[Pd(L-O,S)2] [where HL-O,S = N-(di(butyl/phenyl)carbamothioyl)benzamide] as metal based antiamoebic drug candidates, have been synthesized. Both complexes are characterized in the solid state by FT-IR spectroscopy, TGA and single crystal X-ray study, as well as in solution by other spectroscopic techniques such as (1)H and (13)C NMR, and UV-visible. All these studies confirm the coordination of ligands through oxygen and sulphur atoms upon thioenolization induced delocalization. Complexes adopt cis-configuration in the solid state. Both the complexes and their respective ligands were screened in vitro for antiamoebic activity against HM1:1MSS strain of Entamoeba histolytica by microdilution method and cell viability in response to drugs was checked by using MTT assay. The IC50 values in the range 0.30-0.80 μM for ligands as well as complexes compared to 1.40 for metronidazole along with their similar inhibitory effect on cell viability of HEK293 cells like metronidazole make them promising future antiamoebic drugs.
authors.affiliation: Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee 247667, India. Electronic address: rkmanfcy@iitr.ac.in.
authors.forename: Mannar R
authors.initials: MR
authors.lastname: Maurya
authors.affiliation: Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee 247667, India.
authors.forename: Bhawna
authors.initials: B
authors.lastname: Uprety
authors.affiliation: Departamento de Química Fundamental, Universidade da Coruña, Campus de A Zapateira, 15071 A Coruña, Spain.
authors.forename: Fernando
authors.initials: F
authors.lastname: Avecilla
authors.affiliation: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 100 025, India.
authors.forename: Saba
authors.initials: S
authors.lastname: Tariq
authors.affiliation: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 100 025, India.
authors.forename: Amir
authors.initials: A
authors.lastname: Azam
mesh_terms: D000563:Amebicides / Q000737:chemistry* / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology*; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004748:Entamoeba histolytica / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010165:Palladium / Q000737:chemistry*; D010670:Phenylthiourea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000563:Amebicides; D001549:Benzamides; D056831:Coordination Complexes; C571363:N-(phenylcarbothiol)benzamide; C000606535:bis(N-(dibutylcarbamothioyl)benzamide)palladium(II); C000606534:bis(N-(diphenylcarbamothioyl)benzamide)palladium(II); D010165:Palladium; D010670:Phenylthiourea
keywords: Antiamoebic activity; Crystal structure; NMR spectra; OS donor ligands; Palladium complexes