Synthesis, characterization and biological activity of 4-imino-3-substituted-2-thioxo-1,2,3,4-tetrahydrobenzo[g]pteridine-5,10-dioxide

Abstract

A new series of 4-imino-3-substituted-2-thioxo-1,2,3,4-tetrahydrobenzo[g]pteridine 5,10-dioxide derivatives (3a-s) were prepared by the cycloaddition of alkyl/arylisothiocyanate to 3-aminoquinoxaline-2-carbonitrile-1,4-dioxides derivatives (2a-c). All new compounds gave satisfactory analytical and spectral data in accordance to their assigned structures. Of the tested compounds for glyoxalase-I inhibitory activity, compound 3r has showed the highest activity with an IC₅₀ of 31.5 µM