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

• Published in: European journal of medicinal chemistry Vol. 97; pp. 525 - 537
• Main Author: Krasavin, Mikhail
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 05.06.2015
• Subjects: 2-imidazolines; Animals; Drug Discovery - methods; Humans; Imidazoles - chemistry; Imidazoles - pharmacology; Imidazoline Receptors - metabolism; Molecular Targeted Therapy; Phenotype; Phenotypic biological activity; Privileged structures; Receptors, Adrenergic - metabolism; Scaffolds; Target-specific biological assays; Phenotypic biological activity; 2-imidazolines; Privileged structures; Target-specific biological assays; Scaffolds
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2014.11.028

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. [Display omitted] •Compounds containing 2-imidazoline scaffold display many biological activities.•The review focuses on target-based and phenotypic biological activities.•Many reports fall outside the traditional α/imidazoline receptor domain.•The data available supports the privileged character of 2-imidazolines.