European Journal of Medicinal Chemistry Available online 6 May...

European Journal of Medicinal Chemistry
Available online 6 May 2016
8-Hydroxyquinolines in medicinal chemistry: A structural perspective
Valentina Oliveria, Graziella Vecchioa
Highlights

The interest in 8-hydroxyquinolines has grown exponentially.
8-hydroxyquinoline is an important scaffold in drug design and discovery.
Biological activity of 8-hydroxyquinoline-based systems is reported.
The interaction of 8-hydroxyquinolines with essential metal ions is described.
Postulated mechanisms of action of 8-hydroxyquinoline-based systems are discussed.

Abstract

8-Hydroxyquinolines are heterocyclic compounds characterized by a moderate metal-binding affinity. The interest in 8-hydroxyquinolines has grown exponentially in the last two decades as they are privileged structures for the design of new drug candidates that exert a host of biological effects on various targets.

The study of biological activities such as neuroprotection, anticancer, antibacterial, antifungal activity has been further promoted by the synthetic versatility of 8-hydroxyquinoline, which allows the generation of a large number of derivatives. This includes numerous multifunctional analogues having the metal-binding motif of 8-hydroxyquinoline. In this review, we have summarized 8-hydroxyquinolines, 8-hydroxyquinoline-like compounds, 8-hydroxyquinoline-loaded nanoparticle systems with respect to their biological activities, interaction with metal ions and mechanisms of action.