Synthesis and biological evaluation of new barbituric and thiobarbituric acid fluoro analogs of benzenesulfonamides as antidiabetic and antibacterial agents

摘要

A novel series of benzenesulfonamide derivatives of barbituric and thiobarbituric acids (2-12) were synthesized by condensation and cyclization reactions of various ureido and thioureido derivatives of sulfanilamides. Different substituents have been incorporated at C-5 of barbituric and thiobarbituric acid. Fluoro- and trifluoroacetyl substituents have been installed on various positions and their comparative biological screening was performed with the corresponding non-fluorinated analogs. The synthesized compounds were evaluated for their antimicrobial and antidiabetic activities. Some of the target compounds with fluorine substitution have shown very good antibacterial and antidiabetic activities.