Examining Barbiturate Scaffold for the Synthesis of New Agents with Biological Interest

Abstract

<b>Aim:</b> Barbiturates have a long history of being used as drugs presenting wide varieties of biological activities (antimicrobial, anti-urease and antioxidant). Reactive oxygen species are associated with inflammation implicated in cancer, atherosclerosis and autoimmune diseases. Multitarget agents represent a powerful approach to the therapy of complicated inflammatory diseases. <b>Results:</b> A novel series of barbiturates has been synthesized and evaluated in several <i>in vitro</i> assays. Compound <b>16b</b> (lipoxygenases inhibitor, 55.0 μM) was found to be a cyclooxygenase-2 inhibitor (27.5 μM). Compound <b>8b</b> was profiled as a drug-like candidate. <b>Conclusion:</b> The barbiturate core represents a new scaffold for lipoxygenases inhibition, and the undertaken derivatives show promise as multiple-target agents to combat inflammatory diseases.