Fluorinated Barbituric Acid Derivatives: Synthesis and Bio-activity

Barbituric acid derivatives exert important action on the central nervous system, and recently have found totally new biomedicinal applications in fields such as cancer and AIDS therapy, and protease inhibitors. On the other hand, selective introduction of fluorine into biologically active compounds can either enhance their pharmacological properties or increase their therapeutic efficiency. This review focuses on the synthesis and the biological properties of fluorinated barbituric acid derivatives, which can be divided into three main categories: 1) those bearing a fluorine directly bound in position 5 of the 2,4,6-trioxohexahydro-pyrimidine ring, 2) 5-fluoroalkyl derivatives, and 3) 5-fluoroaryl derivatives.