The method of discovering new drugs is costly, time-consuming, laborious, and associated with a high failure rate. Various techniques have been applied in modern drug discovery to resolve these issues and discover novel pharmacologically active agents. Natural products are one of the sources of drugs that have long been used to treat various illnesses. Kojic acid (KA) is a naturally produced bioactive chemical with a 3-hydroxy-4-pyranone skeleton made by numerous aerobic microbes, such as Aspergillus and Penicillium. KA is a potent tyrosinase inhibitor used in cosmetics to lighten skin by reducing hyperpigmentation. In this review, beyond its cosmetic applications, it exhibits versatile biological activities, including anticancer, antibacterial, antifungal, antioxidant, antiviral, anti-inflammatory, anticonvulsant, anti-Alzheimer's disease, antidiabetic, and metalchelating properties. KA and its analogs have been reported as promising radioprotective agents capable of mitigating the harmful effects of ionizing radiation. By integrating KA with pharmacologically active scaffolds, researchers have developed potent hybrids, such as aminochloroquinoline- KA derivatives, which demonstrate vigorous β-hematin inhibitory activity and significant efficacy against both delicate and resilient strains of P. falciparum to chloroquine. The approach taken to prepare this review article involved collecting, assessing, and synthesizing relevant literature from different databases. This review systematically explores the comprehensive therapeutic potential of KA and its derivatives, including Mannich base, thiazoles, and 1,2,3-triazoles, for various activities, with Michael Adducts and dinuclear ruthenium complexes which exhibits promising antitumor activity. Combining current knowledge will provide a comprehensive foundation for the rational design and development of clinically relevant agents based on KA pharmacophores.
Ram et al. (Thu,) studied this question.