[1] A variety of routes exist for the synthesis of imidazolines,[1][2] with the most common methods involving the condensation of 1,2-diamines (e.g. ethylenediamine) with nitriles or esters.

These metabolites have received considerable attention because of their potent properties such as antitumor, antiviral, and anti-inflammatory activities.

[4] Most bio-active derivatives bear a substituent (aryl or alkyl group) on the carbon between the nitrogen centers.

It is also used in the treatment of dysmenorrhea, hypertensive crisis, Tourette's syndrome and attention deficit hyperactivity disorder (ADHD).

The substitutions on the nitrogen atom in the imidazoline ring provide opportunities for fine-tuning the electronic and steric properties.