| Autor: |
Pertino MW; Instituto de Química de Recursos Naturales, Universidad de Talca, Campus Lircay, Talca 3480094, Chile., F de la Torre A; Department of Medical Physics, School of Medicine and Public Health, University of Wisconsin-Madison, Madison, WI 53705, USA., Schmeda-Hirschmann G; Instituto de Química de Recursos Naturales, Universidad de Talca, Campus Lircay, Talca 3480094, Chile., Vega Gómez C; Centro para el Desarrollo de la Investigación Científica (CEDIC), Manduvirá 635, Asunción CP 1255, Paraguay., Rolón M; Centro para el Desarrollo de la Investigación Científica (CEDIC), Manduvirá 635, Asunción CP 1255, Paraguay., Coronel C; Centro para el Desarrollo de la Investigación Científica (CEDIC), Manduvirá 635, Asunción CP 1255, Paraguay., Rojas de Arias A; Centro para el Desarrollo de la Investigación Científica (CEDIC), Manduvirá 635, Asunción CP 1255, Paraguay., Molina-Torres CA; Servicios de Dermatología, Hospital Universitario 'José E. González', Universidad Autónoma de Nuevo León, Monterrey 64460, NL, Mexico., Vera-Cabrera L; Servicios de Dermatología, Hospital Universitario 'José E. González', Universidad Autónoma de Nuevo León, Monterrey 64460, NL, Mexico., Viveros-Valdez E; Facultad de Ciencias Biológicas, Universidad Autónoma de Nuevo León, San Nicolás de los Garza 66455, NL, Mexico. |
| Abstrakt: |
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 IC 50 values of 19.2, 37.3, 68.7, and 24.7 µM, respectively, outperforming the reference drug benznidazole (IC 50 : 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 (IC 50 : 64.0 µM, SI: 43.0). Additionally, compounds 1a , 1b , and 3f were most effective against Leishmania infantum , with IC 50 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. |
