Synthesis scale up and metabolic studies of natural and synthetic bioactive compounds

Abstract

Despite the richness of Brazilian flora and the broad interest in herbal therapy, almost the whole national market is based in the exotic plant trade. One of the bottlenecks regarding the development of high value products derived from native biodiversity is the lack of clinical and preclinical studies of natural products and synthetic analogs. In recent work leading up to this application, researchers of USP Ribeirão Preto, have made important advances in the understanding the metabolism, in vivo and in vitro, of natural products, as attested by a number of high impact scientific publications. A prerequisite for clinical and compound stability studies is the chemical characterization of active compounds and also the elucidation of possible metabolites. In this context, the application of modern tools of chemical synthesis is essential, enabling the preparation (organic synthesis), characterization and evaluation of both the bioactive molecules and the proposed metabolites. In this project, the demonstrated skills of the Brazilian team in metabolic studies will be supported by the expertise of the University of Durham team in late stage functionalization through C-H activation, synthesis of bioactive natural-product-like heterocyclic compounds and in scaling up chemical process using flow chemistry. Through this collective effort, this joint collaborative research project will be decisive in enabling the development of a modern platform for the metabolic study of natural and synthetic xenobiotics providing great impact in this important area of knowledge. (AU)