Síntese e avaliação biológica de derivados cíclicos de tiopurina e de derivados de quinolinas conjugados com ácido cólico via “click chemistry”

Abstract

This dissertation entitled Synthesis and Biological Evaluation of Cyclical Derivatives of Thiopurine and Quinolines Derivatives Conjugated with Cholic Acid via “Click Chemistry” was divided in two chapters that describe the synthesis of compounds with potential anti-parasitic activity. The first chapter describes the synthesis of 6-mercaptopurine (6-MP) derivatives (Figure below) with the objective obtaining new tricyclic rings via intramolecular N-7 alkylation, as well as obtaining similar the analogs of 6-MP. "Formula disponível no trabalho completo" The second chapter describes the synthesis of 4-aminoquinolines derivatives with a terminal alkyne, as well as cholic acid used to obtain derivatives funcionalized with an azide group in the 3 position. These precursors were quinoline/cholic acid conjugates using click chemistry (Figure below). This work also shows the results of of selected evaluations compounds biological Plasmodium and Leishmania.