Synthesis and trypanocidal activity of novel pyridinyl-1,3,4-thiadiazole derivatives.

Herein, we present the design, synthesis and trypanocidal evaluation of sixteen new 1,3,4-thiadiazole derivatives from N-aminobenzyl or N-arylhydrazone series. All derivatives were assayed against the trypomastigote form of Trypanosoma cruzi, showing IC50 values ranging from 3 to 226 µM, and a better trypanocidal profile was demonstrated for the 1,3,4-thiadiazole-N-arylhydrazones (3a-g). In this series, the 2-pyridinyl fragment bound to the imine subunit of the hydrazine moiety presented pharmacophoric behavior for trypanocidal activity. Compounds 2a, 11a and 3e presented remarkable activity and excellent selectivity indexes. Compound 2a was also active against the intracellular amastigote form of T. cruzi. Moreover, its corresponding hydrochloride, compound 11a, showed the most promising profile, producing phenotypic changes similar to those caused by posaconazole, a well-known inhibitor of sterol biosynthesis. Thus, 1,3,4-thiadiazole derivative 11a could be considered a good prototype for the development of new drug candidates for Chagas disease therapy.

Como realizar uma análise crítica de um artigo científico / Accomplishing a critical analysis of a scientific article

Atualmente, muitos periódicos científicos são publicados; porém, nem todas as informações contidas nestes são confiáveis. Faz-se necessário, então, que os profissionais de saúde adquiram o hábito de realizar uma leitura crítica da literatura científica para que possam julgar a validade dos trabalhos publicados. Neste contexto, o objetivo desse estudo foi auxiliar os leitores a identificar e selecionar artigos com valor científico e ainda analisá-los criticamente. Para este fim, os requisitos necessários para a realização de uma análise crítica da literatura científica foram analisados