Síntese de derivados heterocíclicos como potenciais candidatos a fármacos tuberculostáticos

Abstract

Tuberculosis is a chronic infectious and curable disease caused by the ancient microorganism Mycobacterium tuberculosis. Despite advances in technology, huge scientific knowledge, improvement in quality of life and development of vaccines and drug treatment, the incidence and resistance of Tuberculosis (TB) is increasing worldwide. The World Health Organization (WHO) has been engaged in developing effective strategies and mass monitoring aimed at controlling and eradicating the disease. In this scope, the need to develop new specific antimicrobial drugs has been highlighted. Quinazolines derivatives has shown to be a promising class with several biological and microbiological activities, including activities against Mycobacterium. In another line of research developed in our group, compound PH100, a quinazolinic derivative, was synthesized and demonstrated antibacterial and antibiofilm activities against Staphylococcus aureus and Staphylococcus epidermidis. Due to these antibacterial activity findings, a scientific research has started to explore and identify a possible activity against M. tuberculosis. In this work, five quinazolinic derivatives (PH100, 3a, 3b, 3c and 3d) were synthesized and characterized. A biological evaluation through an inhibition assay using M. tuberculosis H37Rv strains to identify potential anti-TB action in these compounds was performed.