RT info:eu-repo/semantics/article
T1 Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections
A1 Pertino, Mariano Walter
A1 F. de la Torre, Alexander
A1 Schmeda Hirschmann, Guillermo
A1 Vega Gómez, María Celeste
A1 Rolón, Miriam Soledad
A1 Coronel, Cathia Cecilia
A1 Rojas de Arias, Gladys Antonieta
A1 Molina Torres, Carmen A.
A1 Vera Cabrera, Lucio
A1 Viveros Valdez, Ezequiel
AB Background/Objectives: In this study, the efficacy of benzo[h]chromene derivatives as antiprotozoal and antimycobacterial agents was explored. Methods: A total of twenty compounds, including benzo[h]chromene alkyl diesters and benzo[h]chromene-triazole derivatives, were synthesized and tested against Trypanosoma cruzi, Leishmania braziliensis, L. infantum, and strains of Mycobacterium abscessus and Mycobacterium intracellulare LIID-01. Notably, compounds 1a, 1b, 2a, and 3f exhibited superior activity against Trypanosoma cruzi, with IC50 values of 19.2, 37.3, 68.7, and 24.7 µM, respectively, outperforming the reference drug benznidazole (IC50: 54.7 µM). Results: Compounds 1b and 3f showed excellent selectivity indices against Leishmania braziliensis, with SI values of 19 and 18, respectively, suggesting they could be potential alternatives to the commonly used, but more selective, miltefosine (IC50: 64.0 µM, SI: 43.0). Additionally, compounds 1a, 1b, and 3f were most effective against Leishmania infantum, with IC50 values of 24.9, 30.5, and 46.6 µM, respectively. Compounds 3f and 3h were particularly potent against various Mycobacterium abscessus strains, highlighting their significance given the inherent resistance of these bacteria to standard antimicrobials. Conclusions: The sensitivity of Mycobacterium intracellulare LIID-01 to these compounds also underscored their potential in managing infections by the Mycobacterium avium–intracellulare complex.
PB Multidisciplinary Digital Publishing Institute
YR 2024
FD 2024-10-16
LK http://hdl.handle.net/20.500.14066/4476
UL http://hdl.handle.net/20.500.14066/4476
LA eng
NO Pertino, M. W., F. de la Torre, A., Schmeda Hirschmann, G., Vega Gómez, C., Rolón, M., Coronel, C., Rojas de Arias, A., Molina Torres, C. A., Vera Cabrera, L., & Viveros Valdez, E. (2024). Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections. Pharmaceuticals, 17(10), Artículo 1375. https://doi.org/10.3390/ ph17101375
NO Correspondence: mwalter@utalca.cl; Tel.: +56-71-2418866
NO This article belongs to the Special Issue Click Reactions in Medicinal Chemistry II.
NO Consejo Nacional de Ciencia y Tecnología
DS MINDS@UW
RD 23-dic-2024