Síntese e avaliação biológica de derivados 4-aminoquinolínicos e 4-mercaptoquinolínicos

Abstract

This work entitled Synthesis and Biological Evaluation of 4-Aminoquinolines and 4-Mercaptoquinolines Derivatives is divided in two parts and describes the synthesis of quinolinic compounds coupled to molecules and / or heterocyclic compounds with biological activity. The first part deals with obtaining of 4-aminoquinolines derivatives. It presents the synthesis of 20 substances made by the coupling of sulfanilamide, isoniazid and 4-aminosalicylic acid derivatives to the quinolinic nucleus. The second part deals with obtaining of 4-mercaptoquinolines derivatives to obtain 12 substances with the quinolinic nucleus coupled to other heterocyclic (2-mercaptobenzothiazole and 4-mercaptopyridine). Of the 32 substances synthesized, 11 are new and all were properly characterized by spectroscopic techniques. The compounds were submitted to the biological evaluation against parasites that cause leishmaniasis and pathogenic Gram-positive and Gram-negative bacteria, as well as cytotoxicity tests. Considering the 15 substances tested, 13 were not cytotoxic at the concentrations evaluated, and 11 showed some biological activity, either in promastigotes of the Leishmania genus or pathogenic bacteria.