Anti-Mycobacterium tuberculosis activity of platinum(II)/N,N-disubstituted-N′-acyl thiourea complexes

• Pt(II)/N,N-disubstituted-N′-acyl thiourea complexes with general formula [Pt(dppf)(Ln)]PF6 were obtained.
• The complexes exhibit anti-Mycobacterium tuberculosis activities.
• Complexes with small ligand Ln present higher activity than those with big Ln.
• The complexes [Pt(dppf)(Ln)]PF6, with exhibit anti-Mycobacterium tuberculosis activity in the same order of the ethambutol.

Synthesis, characterization and anti-Mycobacterium tuberculosis assays of new platinum(II)/dppf/N,N-disubstituted-N′-acyl thiourea complexes with general formulae [Pt(dppf)(L)]PF6, [dppf = 1,1′-bis(diphenylphosphino)ferrocene; L = N,N-disubstituted-N′-acyl thioureas] is reported. The complexes were characterized by elemental analysis, molar conductivity, IR, NMR (1H, 13C and 31P{1H}) spectroscopy. The spectroscopic data are consistent with the complexes containing one dppf and one O, S chelated ligand. The crystal structures of complexes with N,N-diphenyl-N′-benzoylthiourea (L4), N,N-diethyl-N′-furoylthiourea (L5) and N,N-diphenyl-N′-(thiophene-2-carbonyl)thiourea (L8) were determined by X-ray crystallography, confirming the coordination of the ligands with the metal through sulfur and oxygen atoms, forming distorted square-planar structures. The complexes were screened with respect to their anti-M. tuberculosis activity (H37Rv ATCC 27294).

The syntheses of the complexes with general formulae [Pt(dppf)(L)]PF6 (L = N,N-disubstituted-N′-acyl thiourea and dppf = 1,1′-(diphenylphosphine)ferrocene; L = N,N-disubstituted-N′-acyl thioureas] are reported. The complexes were characterized by elemental analysis, molar conductivity, IR, NMR (1H, 13C and 31P{1 H}) spectroscopy and X-ray spectroscopy. The complexes showed anti-Mycobacterium tuberculosis activity as good as the ethambutol, a first-line drug used in the tuberculosis treatment.Figure optionsDownload as PowerPoint slide