Microbial resistance (MR) and cancer are global healthcare pitfalls that have caused millions of deaths and pose a significant pharmaceutical challenge, with clinical cases increasing. Thioureas are preferred structures in medicinal chemistry, chemosensors, and organic synthesis platforms. In fact, thiourea (TU) moieties serve as a common framework for several medications and bioactive substances, demonstrating a wide range of therapeutic and pharmacological accomplishments. The integration of the thiourea moiety into a diverse range of organic molecules has resulted in very flexible compounds with widespread uses in medicinal chemistry. Moreover, for over a century, TU and its metal complexes have been characterized for their biological activity. Finally, we provide an assessment and future outlook of different organo-thiourea derivatives, from the very beginning to the most recent discoveries in medicinal activity.

Coordination compounds offer a flexible framework for the thoughtful design of novel therapeutic-metallodrugs because of the unique properties of metal ions, such as their ability to coordinate with a wide range of organic ligands, variable oxidation states, a wide range of geometries, and coordination numbers. The pharmaceutical potential of a metal ion and associated substances is validated by the prevalence of various disease states linked to a metal ion's excess or deficiency within the biological system. Researchers have sought more selective, efficacious metallodrugs that cause fewer adverse effects. Attempts have resulted in considering a large range of organic ligands, preferably polydentate ligands with demonstrated biological activity, and a large range of metals from the periodic table, primarily from the d-block. In this review, we have outlined the key coordination complexes comprising N-, O-, and S-donor ligands reported in the last six years to demonstrate the potential applications of these metallo-organic complexes. The synthetic pathways of ligands, their complexes, and their potential for therapeutic applications are highlighted.

Two series of polydentate N,O,S-ligands containing thiourea fragments attached to a p-cresol scaffold, unsymmetrical mono-acylated bis-amines and symmetrical bis-thioureas, are obtained by common experiments. It is observed that the reaction output is strongly dependent on both bis-amine and thiocarbamic chloride substituents. The products are characterized by 1D and 2D NMR spectra in solution and by single crystal XRD. A preliminary study on the coordination abilities of selected products is performed by ITC at around neutral media.