Synthesis of Isoxazolic analogues derivatives of Grandisin and Veraguensin neolignans with anti-leishmania and antitrypanosomal activities

Abstract

The search for new biologically active compounds and, consequently, with possible use in the treatment of various diseases has been increasing in recent decades. In this study we used the bioisosterism as molecular modification strategy of the neoliganans grandisin and veraguensina what are the natural compounds with biological activity against neglected diseases. The isoxazolic heterocyclic ring was chosen as substituent of the tetrahidrofuranic rings found in these neolignans. In order to obtain more potent compounds with fewer side effects and better physicochemical characteristics, in this study were synthesized 12 isoxazolic analogues, these were sent for antileishmania and anti-trypanosomal biological activity testing, which provided us important informations about the structure-activity relationship.