The introduction of the complex sulfone derivatives marked a considerable advance in the treatment of leprosy, but it also meant a period of some confusion while the various kinds of derivatives were on trial. The period of trial has, in the main, ended by the acceptance of the majority of the parent substance, DDS, as the drug of choice. It is noted, however, that at the BELRA conference on su...

Xi, R., Pun, I., Menezes, S., Fouani, L., Kalinowski, D., Huang, M., Zhang, X., Richardson, D., Kovacevic, Z. (2017). Novel Thiosemicarbazones Inhibit Lysine-Rich Carcinoembryonic Antigen-Related Cell Adhesion Molecule 1 (CEACAM1) Coisolated (LYRIC) and the LYRIC-Induced EpithelialMesenchymal Transition via Upregulation of N-Myc Downstream-Regulated Gene 1 (NDRG1). Molecular Pharmacology, 91(5)...

A quantitative structure-activity relationship analysis was employed to explore the relationship between the molecular structure of thiosemicarbazone analogues and the inhibition of the cysteine protease cruzain, a validated target for Chagas' disease treatment. A data set containing 53 thiosemicarbazone derivatives was used to produce a quantitative model for activity prediction of unknown com...

New imidazole derived thiosemicarbazones and hydrazones were prepared by condensation of 4(5)-imidazole carboxaldehyde, 4-(1H-imidazole-1-yl)benzaldehyde and 4-(1H-imidazole-1-yl)acetophenone with a thiosemicarbazide or hydrazide. All compounds were characterized by quantitative elemental analysis, IR and NMR techniques. Eight structures were determined by single crystal X-ray diffraction. The ...

The chelating behavior of the thiosemicarbazone derivatives of 2-hydroxy-8-R-tricyclo[7.3.1.0.(2,7)]tridecane-13-one (where R = H, CH3, C6H5) towards Co(II), Ni(II) and Cu(II) has been investigated by elemental analysis, molar conductivity measurements, UV-VIS, IR, ESR spectroscopy and thermal studies. It was deduced from the experiments performed that the ligands coordinate to metal ions in di...

In the title compound, [Fe(2)Zn(C(5)H(5))(2)(C(7)H(7)N(3)S)(2)], the Cp rings of each ferrocene residue have a nearly eclipsed conformation. The two thio-semicarbazone ligands each coordinate the Zn atom in a bidentate mode via the N and S atoms, thereby defining a distorted tetra-hedral environment. N-H⋯S, N-H⋯N, C-H⋯S and C-H⋯N intra- and intermol-ecular inter-actions connect the mol-ecules i...

A series of 2-acylpyridine thiosemicarbazones was evaluated in vitro against a chloroquine-resistant Plasmodium falciparum strain. Antimalarial activity was assessed by the inhibition of uptake of [G-3H]hypoxanthine by the parasites. Among the mono- and disubstituted derivatives tested, 13 of 17 had 50% inhibitory doses of less than 10 ng/ml. Increasing the size of the ring at N4 from four to f...

The aims of this study were to synthesize a series of thiosemicarbazones and their thiazole derivatives, to investigate their cytotoxic activity against three human cancers and normal (Vero cells) cell lines, and to evaluate the pro-apoptotic potential of the most active compounds. Materials and Methods: The thiosemicarbazones were obtained by reacting an aromatic aldehyde with thiosemicarbazid...