Abstract
Although organic compounds account for more than 99% of currently approved clinical drugs, the established clinical use of cisplatin in cancer or auranofin in rheumatoid arthritis have paved the way to several research initiatives to identify metal-based drugs for a wide range of human diseases. Nitrogen and sulfur donor ligands, characterized by different binding motifs, have been the subject in recent years of one of the main research areas in coordination chemistry. Among the nitrogen/sulfur compounds, very little is known about thiocarbohydrazones (TCH), the higher homologues of the well-known thiosemicarbazones (TSC), and their metal complexes. The extra hydrazine moiety provides the ligands of variable metal binding modes, structural diversity and promising biological implications. The interesting coordination chemistry of TCH has mainly been focused on symmetric derivatives, which are relatively simple to synthesize while few examples of asymmetric ligands have been reported. This informative review on TCHs and their metal complexes will be helpful for improving the design of metal-based pharmaceuticals for applications ranging from anticancer to antinfective therapy.
Highlights
The use of metals for medicinal purposes has been exploited since very ancient times; for instance, silver has been used as a disinfectant agent for water and milk for thousands of years [1]
TCHs derived from salycilaldehyde, the results of this study indicate the importance of lipophilicity for the antimicrobial activity of thiocarbonohydrazones ligand
The ligand and its complexes were screened for antibacterial activity against Escherichia coli, Staphylococcus aureus, Bacillus aureus and Aspergillus niger and antifungal activity towards Candida albicans: the ligand is active against bacteria tested in the present study, but the promising results were observed for the copper complexes against all bacterial and fungal strains
Summary
The use of metals for medicinal purposes has been exploited since very ancient times; for instance, silver has been used as a disinfectant agent for water and milk for thousands of years [1]. The most important impulse to the research of metal-based drugs with medicinal properties came from the serendipitous discovery of the antitumor features of cisplatin by Rosenberg. Until reports concerned the synthesis and characterization of ligands and their complexes with transition metals were reported Recently it was understood the potential of these systems: TCHs are able to act as metal-based drugs and their biological activities were investigated. Coordinate metals metals and the remarkable biological properties of the resulting complexes, no general coordinate survey on the employment of TCHs as suitable ligand for the synthesis of metal-based drugs has yet reported. Together with the novelty represented by these systems and the numerous fields of application, it is not possible to identify a unique action mechanism: each combination (metal cation/TCHs backbone/field of employ) can give rise to a different mechanism of action, which has only been deeply investigated in a few cases; when available, clear indications of the action mechanism of the TCHs metal complexes are reported in the text
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