A multistep and diversity-oriented synthetic route aiming at the A3 coupling/domino cyclization of o-ethynyl anilines, aldehydes and s-amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross-coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomponent reaction underwen...
Despite excellent drug discovery programs and unprecedent commitment to eliminate malaria, this protozoan disease remains a major cause of mortality and morbidity worldwide, and specially in developing nations. Apart from socio-economic issues, drug-resistance seems to be the major causing factor for the malaria incidence in these countries. This project aimed to disclose new leads that are active against drug-...