At present, diseases resulting from various reasons have been causing deadly fears to humans
and previously incogitable losses to health. Meanwhile, the patient compliance has been weakening
because of drug resistance and serious drug adverse effects. There is therefore an urgent need for
the development of novel structural agents. Rhodanine derivatives have exhibited wide biological activities,
as well as significant industrial applications, which suggests that rhodanine heterocycle represents
a key structural motif in heterocyclic chemistry and occupies a prominent position in drug discovery.
Here, we review some deadly defects of clinical medicines to the therapy of diseases and important
advances on rhodanine derivatives in drug researches (e.g. as anti-diabetic, anti-viral, antiinflammatory,
anti-microbial, anti-tumor agents and inhibitors for Alzheimer Disease), indicating that
rhodanine heterocycle could be used as a significant pharmacophore to develop novel pharmacological
active molecules. It is believed that the review is of importance for new ideas in the development of
and rational designs of rhodanine-based drugs.