Azole inhibitors of mushroom and human tyrosinases: Current advances and prospects of drug development for melanogenic dermatological disorders

Eur J Med Chem. 2022 Jun 9;239:114525. doi: 10.1016/j.ejmech.2022.114525. Online ahead of print.ABSTRACTAzoles are a famous and promising class of drugs for treatment of a range of ailments especially fungal infections. A wide variety of azole derivatives are also known to exhibit tyrosinase inhibition, some of which possess promising activity with potential for treatment of dermatological disorders such as post-inflammatory hyperpigmentation, nevus, flecks, melasma, and melanoma. Recently, thiazolyl-resorcinol derivatives have demonstrated potent human tyrosinase inhibition with a safe and effective therapeutic profile for treatment of skin hyperpigmentation in humans, which are currently under clinical trials. If approved these derivatives would be the first azole drugs to be used for treatment of skin hyperpigmentation. Although the scientific literature has been witnessing general reviews on tyrosinase inhibitors to date, there is none that specifically and comprehensively discusses azole inhibitors of tyrosinase. Appreciating such potential of azoles, this focused review highlights a wide range of their derivatives with promising mushroom and human tyrosinase inhibitory activities and clinical potential for treatment of melanogenic dermatological disorders. Presently, these disorders have been treated with kojic acid, hydroquinone and other drugs, the design and development of which are based on their ability to inhibit mushroom tyrosinase. The active sites of mushroom a...
Source: European Journal of Medicinal Chemistry - Category: Chemistry Authors: Source Type: research