Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections
Correspondence: mwalter@utalca.cl; Tel.: +56-71-2418866
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| Eará dahkkit: | , , , , , , , , |
| Materiálatiipa: | article |
| Giella: | eaŋgalasgiella |
| Almmustuhtton: |
2024
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| Fáttát: | |
| Liŋkkat: | https://doi.org/10.3390/ph17101375 http://hdl.handle.net/20.500.14066/4476 |
| Fáddágilkorat: |
Eai fáddágilkorat, Lasit vuosttaš fáddágilkora!
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| _version_ | 1870612072806481920 |
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| author | Pertino, Mariano Walter |
| author2 | F. de la Torre, Alexander Schmeda Hirschmann, Guillermo Vega Gómez, María Celeste Rolón, Miriam Soledad Coronel, Cathia Cecilia Rojas de Arias, Gladys Antonieta Molina Torres, Carmen A. Vera Cabrera, Lucio Viveros Valdez, Ezequiel |
| author2_role | author author author author author author author author author |
| author_browse | Coronel, Cathia Cecilia F. de la Torre, Alexander Molina Torres, Carmen A. Pertino, Mariano Walter Rojas de Arias, Gladys Antonieta Rolón, Miriam Soledad Schmeda Hirschmann, Guillermo Vega Gómez, María Celeste Vera Cabrera, Lucio Viveros Valdez, Ezequiel |
| author_facet | Pertino, Mariano Walter F. de la Torre, Alexander Schmeda Hirschmann, Guillermo Vega Gómez, María Celeste Rolón, Miriam Soledad Coronel, Cathia Cecilia Rojas de Arias, Gladys Antonieta Molina Torres, Carmen A. Vera Cabrera, Lucio Viveros Valdez, Ezequiel |
| author_role | author |
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| bitstream.url.fl_str_mv | http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/6/Exploring%20benzo%5bh%5dchromene%20derivatives%20as%20agents%20against%20protozoal%20and%20mycobacterial%20infections.jpg http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/1/Exploring%20benzo%5bh%5dchromene%20derivatives%20as%20agents%20against%20protozoal%20and%20mycobacterial%20infections.pdf http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/5/Supplementary%20Material_Supplementary%20File%201.pdf http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/2/license_rdf http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/3/license.txt http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/4/Exploring%20benzo%5bh%5dchromene%20derivatives%20as%20agents%20against%20protozoal%20and%20mycobacterial%20infections.pdf.txt http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/7/Supplementary%20Material_Supplementary%20File%201.pdf.txt |
| dc.creator.none.fl_str_mv | Pertino, Mariano Walter F. de la Torre, Alexander Schmeda Hirschmann, Guillermo Vega Gómez, María Celeste Rolón, Miriam Soledad Coronel, Cathia Cecilia Rojas de Arias, Gladys Antonieta Molina Torres, Carmen A. Vera Cabrera, Lucio Viveros Valdez, Ezequiel |
| dc.date.accessioned.none.fl_str_mv | 2024-11-09T13:54:38Z |
| dc.date.available.none.fl_str_mv | 2024-11-09T13:54:38Z |
| dc.date.issued.none.fl_str_mv | 2024-10-16 |
| dc.format.extent.es.fl_str_mv | 12 páginas |
| dc.identifier.citation.en.fl_str_mv | 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 |
| dc.identifier.doi.es.fl_str_mv | 10.3390/ ph17101375 |
| dc.identifier.essn.es.fl_str_mv | 1424-8247 |
| dc.identifier.other.es.fl_str_mv | https://doi.org/10.3390/ph17101375 |
| dc.identifier.uri.none.fl_str_mv | http://hdl.handle.net/20.500.14066/4476 |
| dc.language.iso.es.fl_str_mv | eng |
| dc.publisher.es.fl_str_mv | Multidisciplinary Digital Publishing Institute |
| dc.rights.*.fl_str_mv | Atribución 4.0 Internacional |
| dc.rights.accessRights.es.fl_str_mv | info:eu-repo/semantics/openAccess |
| dc.rights.uri.*.fl_str_mv | http://creativecommons.org/licenses/by/4.0/ |
| dc.subject.other.es.fl_str_mv | Antiprotozoal activity Benzo[h]chromene Click chemistry Mycobacterial infections |
| dc.title.es.fl_str_mv | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| dc.type.es.fl_str_mv | info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
| description | Correspondence: mwalter@utalca.cl; Tel.: +56-71-2418866 |
| eu_rights_str_mv | openAccess |
| format | article |
| id | CONACYT_e193c2b9fc3995f66ec74d69d8965270 |
| identifier_str_mv | 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 10.3390/ ph17101375 1424-8247 |
| language | eng |
| network_acronym_str | CONACYT |
| network_name_str | Repositorio Institucional CONACYT |
| oai_identifier_str | oai:repositorio.conacyt.gov.py:20.500.14066/4476 |
| publishDate | 2024 |
| publishDateSort | 2024 |
| repository.mail.fl_str_mv | repositorio.institucional@conacyt.gov.py |
| repository.name.fl_str_mv | Repositorio Institucional CONACYT |
| repository_id_str | |
| rights_invalid_str_mv | Atribución 4.0 Internacional http://creativecommons.org/licenses/by/4.0/ |
| spelling | e80ec11b-1c10-42ca-b589-ffcf1a4d84636005555d912-b1ac-462d-8d3b-218433dc67796002c2eb3f4-15b5-44ec-9df1-c17ca59be99360011456000000-0001-6291-431610066003086009976000000-0002-6207-187098dcdbfb-ca39-4ef2-96b5-c02d53972e01600ce486c58-f75c-423f-875b-d974c3c8df5660029317add-b5ff-45ef-8bee-9db69958fb1e6002024-11-09T13:54:38Z2024-11-09T13:54:38Z2024-10-16Pertino, 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/ ph17101375https://doi.org/10.3390/ph17101375http://hdl.handle.net/20.500.14066/447610.3390/ ph171013751424-8247Correspondence: mwalter@utalca.cl; Tel.: +56-71-2418866This article belongs to the Special Issue Click Reactions in Medicinal Chemistry II.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.Consejo Nacional de Ciencia y TecnologíaPrograma Paraguayo para el Desarrollo de la Ciencia y Tecnología. Programa Nacional de Incentivo a los Investigadores12 páginasengMultidisciplinary Digital Publishing InstituteAtribución 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccess© 2024 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/).Antiprotozoal activityBenzo[h]chromeneClick chemistryMycobacterial infectionsExploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infectionsinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion10Pharmaceuticals17Pertino, Mariano WalterF. de la Torre, AlexanderSchmeda Hirschmann, GuillermoVega Gómez, María CelesteRolón, Miriam SoledadCoronel, Cathia CeciliaRojas de Arias, Gladys AntonietaMolina Torres, Carmen A.Vera Cabrera, LucioViveros Valdez, EzequielTHUMBNAILExploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections.jpgExploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections.jpgArtículo científicoimage/jpeg968042http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/6/Exploring%20benzo%5bh%5dchromene%20derivatives%20as%20agents%20against%20protozoal%20and%20mycobacterial%20infections.jpgf51b2c25a08b9a9e9a0efa8c8718bb99MD56ORIGINALExploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections.pdfExploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections.pdfArtículo científicoapplication/pdf652957http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/1/Exploring%20benzo%5bh%5dchromene%20derivatives%20as%20agents%20against%20protozoal%20and%20mycobacterial%20infections.pdf7b3abf88d6a02c9fa4248ad813267b15MD51Supplementary Material_Supplementary File 1.pdfSupplementary Material_Supplementary File 1.pdfArchivo complementario 1application/pdf1191013http://repositorio.conacyt.gov.py/bitstream/20.500.14066/4476/5/Supplementary%20Material_Supplementary%20File%201.pdf681c366850560261bb9ec244d1dee7a2MD55CC-LICENSElicense_rdflicense_rdfapplication/rdf+xml; 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| spellingShingle | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections Pertino, Mariano Walter Antiprotozoal activity Benzo[h]chromene Click chemistry Mycobacterial infections |
| status_str | publishedVersion |
| title | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| title_full | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| title_fullStr | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| title_full_unstemmed | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| title_short | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| title_sort | Exploring benzo[h]chromene derivatives as agents against protozoal and mycobacterial infections |
| topic | Antiprotozoal activity Benzo[h]chromene Click chemistry Mycobacterial infections |
| url | https://doi.org/10.3390/ph17101375 http://hdl.handle.net/20.500.14066/4476 |