Biologically active compounds based on the privileged 2-imidazoline scaffold: The world beyond adrenergic/imidazoline receptor modulators

Abstract

2-Imidazolines are well known as pharmacophores for various isoforms of adrenergic (α) and imidazoline (I) receptors. The biological activities exerted through the modulation of these targets, mostly in the central nervous system, have found utility in the development of many drug candidates - and even marketed drugs - for hypertension, diabetes and various CNS disorders. However, there is a growing evidence for the general privileged character of the 2-imidazoline scaffold, considering the documented success in the development of numerous biologically active compounds acting outside of the α/I receptor domain. In this review, we provide an overview of these, less traditional areas of medicinal applications of 2-imidazolines.

Keywords: 2-imidazolines; Phenotypic biological activity; Privileged structures; Scaffolds; Target-specific biological assays.