SEMINARIO QUÍMICA ORGÁNICA 19-5-25
EXPOSITOR: Lic. Matías Krivoy
TÍTULO: "Synthesis and in vitro and in silico studies of 1H- and 2H-1,2,3-triazoles as antichagasic agents"
FUENTE: Thais B. Silva et al. Bioorganic Chemistry, 2021, 116, 105250. https://www.sciencedirect.com/science/article/pii/S0045206821006271
DÍA, HORA y LUGAR: Lunes 19 de mayo de 2025, 14:00 h, Aula 18 y virtual.
Modalidad virtual, Link: meet.google.com/hjn-ygro-twf (Plataforma MEET GOOGLE)
Resumen: 1,2,3-triazole heterocycles stand out in medicinal chemistry for having great structural diversity and bioactivities. In this study, two series of triazoles were synthesized. One was obtained by the 1,3-dipolar cycloaddition reaction between ethyl cyanoacetate and several phenyl azides forming 1H-1,2,3-triazoles and the other by rearrangement of Dimroth forming and 2H-1,2,3-triazoles. Both series were shown to be active against the epimastigote form of Trypanosoma cruzi. The 1,2,3-triazoles 16d (S.I. between 100 and 200), 17d and 16f (S.I. > 200) were the most active compounds and capable of breaking the plasma membrane of trypomastigotes acting on CYP51 and inhibiting ergosterol synthesis. Candidate 16d exhibited the best and most favorable profile when interacting with CYP51.
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