The broad and potent activity of 2-thioxo-imidazolidin-4-one (2-thiohydantoin) has established it as one of the biologically important scaffolds. This article highlights the medicinal chemistry investigations in search for novel 2- thioxo-imidazolidin-4-one derivatives with promising biological activities. New 2-thioxo-imidazolidin-4-one derivatives contain diaryl, triaryl, pyrimidine, cycloalkylamines and glucopyranosyl substituents and their aryl and halogen and alkyl derivatives, and other substituent with varied the monocyclic (thiadiazole, sulfadiazole) heterocycles linked directly or through alkyl chain with the imidazolidine nucleus. Recently obtained 2-thioxo-imidazolidin-4-one derivatives exhibit promising antibacterial, antifungal, anticancer, anti-inflammatory and many more biological activities. This review shows current tendency in the 2-thioxo-imidazolidin-4-one synthesis and reveals the 2-thioxo-imidazolidin-4-one core to be potent pharmacophoric moiety.
Keywords: medicinal chemistry, biologically active heterocyclic compounds, scaffold, thiocarbonyl group, antithyroidal, Cterminal protein sequencing, antimicrobial, Cterminal protein sequencing [, human immunodeficiency virus (HIV), anti-ulcer and anti-inflammatory agents