Cinética bactericida de uma nova molécula benzofuroxânica combinada com antibióticos utilizados para o tratamento de tuberculose

• Autor(a) principal: Ribeiro, Camila Maríngolo [UNESP]
• Data de Publicação: 2016
• Tipo de documento: Trabalho de conclusão de curso
• Idioma: por
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://hdl.handle.net/11449/203799; http://www.athena.biblioteca.unesp.br/exlibris/bd/capelo/2019-05-20/000886681.pdf
• topic: Tuberculose; Antibacterianos; Medicamentos - Desenvolvimento; Mycobacterium tuberculosis; Drug development

Tuberculosis (TB) is an infectious disease that kills more people in the world, 9.6 million people affected by 2014, and 1.5 million deaths. The major aggravating factor in this scenario is the emergence of antibiotic-resistant strains available for treatment. To find new potential anti-TB molecules, in partnership with the Laboratory of Research and Development of Medicines, a library of molecules based on the furoxanic and benzofuroxanic nuclei was synthesized. A minimal inhibitory concentration and a cytotoxicity of the molecules of this library were determined. To evaluate the profile of the three most prominent molecules (14c, PJ5 and PJ21), a bactericidal kinetics methodology was used. The molecules 14c and PJ21 had a bactericidal effect superior to the antibiotics used in the therapy. The PJ 5 molecule is bacteriostatic and has the highest index of selectivity, so it was selected to be evaluated in combination with antibiotics used in anti-TB therapy. The results of the combinations were a synergistic effects with isoniazid, rifampicin and amikacin, and an early bactericidal effect with MOX, and the inoculum was completely eliminated with all combination of PJ5 with antibiotic. Anti-TB therapy is always a drugs association, antibiotics that have a synergistic effect when combined with others stand out as potential future drugs. The potentiating effect observed for PJ5 suggests that it can be observed with other molecules of the same chemical class...