: Infectious diseases are among the leading causes of death worldwide, especially in developing countries. The historical lack of interest of the pharmaceutical industry in developing new drugs against many of these diseases, such as tuberculosis, leishmaniasis, Chagas disease, sleeping sickness, and fungal infections, has left millions of individuals dependent on old treatments that are often ineffective and present different adverse effects. In this sense, new substances against these diseases must be identified. A class of substances that has stood out in the search for new drugs against these diseases is azole derivatives. Within this class, the 3-nitro-1,2,4-triazole nucleus has attracted increasing interest due to its potential, specifically when compared to the 1,2,4-triazole nucleus without the presence of the nitro group, and also in relation to the 2-nitroimidazole nucleus, showing greater potency and selectivity against different etiological agents. This is even more relevant considering that 3-nitro-1,2,4-triazolic substances can promote their activity through different mechanisms of action, such as the inhibition of ergosterol biosynthesis and also via activation by the nitroreductase enzyme, which can avoid the development of cross-resistance. Therefore, in this review, the medicinal chemistry of nitrotriazoles is discussed through the analysis of their potential in terms of biological activity against the etiological agents of several diseases, such as Chagas disease, sleeping sickness and leishmaniasis, caused by kinetoplastid parasites, tuberculosis, caused by the mycobacteria Mycobacterium tuberculosis, and against different species of pathogenic fungi. In addition, aspects related to enzymatic activities, molecular modeling and organic synthesis of these substances are also addressed.

Fluconazole is an azolic second-generation antifungal drug and is part of the National List of Essential Drugs (RENAME) of the Brazilian Ministry of Health. It is considered as first choice for the treatment of some opportunistic fungal infections and also applied in the AIDS treatment program as prophylactic therapy to avoid these infections. Due to the importance of fluconazole for the Brazilian Health System (SUS), it is strategic the domain of its obtaining process. Thus, improvements in the synthesis of this substance are also of special interest. In this work, many changes were proposed and carried out in the original fluconazole synthetic route, aiming to increase yield and using solvents and processes with a lower environmental impact. With these optimizations, the overall yield achieved was 53%, which is about 10 times higher than that of the original process. ResumoO fluconazol é um antifúngico da classe dos azóis de segunda geração, sendo integrante da Relação Nacional de Medicamentos Essenciais (RENAME) do Ministério da Saúde do Brasil. Este fármaco é considerado como de primeira escolha para o tratamento de algumas infecções fúngicas oportunistas e também no programa de tratamento da AIDS, como terapia profilática para evitar estas infecções. Devido à importância do fluconazol para o sistema único de saúde (SUS), é estratégico para o Brasil o domínio de seu método de obtenção e, desta forma, melhorias na síntese desta substância também são de especial interesse. Neste trabalho foram propostas e realizadas diversas alterações na rota original do fluconazol, buscando o aumento do rendimento e utilizando solventes e processos de menor impacto ambiental. Com estas otimizações, o rendimento global alcançado foi de 53%, que é cerca de 10 vezes superior ao processo original. Palavras-chave:Fluconazol; síntese; otimização.