Study On Design And Synthesis Of Catalpalactone Analogues And Small Motecule Inhibitors Of Fatty Acid Binding Protein And Biological Activities

In this paper, analogues based on natural compound catalpalactone have been synthesized to discover new antitumor candidate agents. The research of small molecule inhibitors of Fatty Acid Binding Protein design, synthesis and biological activity made full use of traditional medicinal chemistry design theory and computer virtual screening method to expect better active compounds.1. Catalpalactone Analogues : Design, Synthesis and Biological EvaluationPhthalide compounds have a wide range of physiological activities, the state a class of drugs butylphthalide is a phthalide derivatives which is used to treat ischemic cerebrovascular disease, improve the cerebral microcirculation, improve neurological deficits, also asthma , anticonvulsant, inhibit platelet aggregation. This paper designed series of Phthalide derivatives based on the structural of catalpalactone and we got 10 analogues through changing the six-lactone ring. We also study the influence on the structure-activity relationship by changing six-lactone ring and substitution in benzene ring to get better active compounds.2. Design, Synthesis and Biological activity of small molecule inhibitors of Fatty Acid Binding ProteinFatty acid binding protein (FABP4) inhibitor for the treatment of obesity, diabetes, arteriosclerosis and fat have caused widespread concern.In recent years, the old medicine new drug development has the new trend. Based on the consideration of new target, we transformed the structure of benzbromarone to get compounds with better inhibitory activity.