Imidazole

Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG₂ and PGH₂) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL^Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease^[1][2][3].
In Vitro: Imidazole (0.01-100 μM, 48 h) shows no inhibitory activityis, but imidazole derivatizations shows significant inhibitory effects in different tumor cell lines^[1].
Imidazole (0.01-100 μM, 48 h) has a weak affinity for both EGFR and HER2, whereas the derivatization improves their affinity for these receptors in tumor cells^[1].
In Vivo: Imidazole (50 pg/ml, infusion) and similar compounds are selective inhibitors of the conversion of endoperoxides into thromboxanes^[3].