Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones

Detalhes bibliográficos
Autor(a) principal: Bento, Clara M.
Data de Publicação: 2023
Outros Autores: Silva, Ana Teresa, Mansano, Bruno, Aguiar, Luísa, Teixeira, Cátia, Gomes, Maria Salomé, Gomes, Paula, Silva, Tânia, Ferraz, Ricardo
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10400.22/22536
Resumo: This work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutical ingredients (API-OSs), as those herein disclosed, hold promise as cost-effective formulations with improved features over their parent drugs, thus enabling the mitigation of some of their shortcomings. For instance, in the specific case of clofazimine, its poor solubility severely limits its bioavailability. As compared to clofazimine, the clofazimine-derived OSs now reported have improved solubility and thermostability, without any major deleterious effects on the drug’s bioactivity profile.
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spelling Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolonesAntibioticsGUMBOSIonic liquidsMycobacteriumOrganic saltsRepurposingRescuingThis work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutical ingredients (API-OSs), as those herein disclosed, hold promise as cost-effective formulations with improved features over their parent drugs, thus enabling the mitigation of some of their shortcomings. For instance, in the specific case of clofazimine, its poor solubility severely limits its bioavailability. As compared to clofazimine, the clofazimine-derived OSs now reported have improved solubility and thermostability, without any major deleterious effects on the drug’s bioactivity profile.MDPIRepositório Científico do Instituto Politécnico do PortoBento, Clara M.Silva, Ana TeresaMansano, BrunoAguiar, LuísaTeixeira, CátiaGomes, Maria SaloméGomes, PaulaSilva, TâniaFerraz, Ricardo2023-03-17T17:05:46Z2023-01-112023-01-11T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10400.22/22536engBento, C. M., Silva, A. T., Mansano, B., Aguiar, L., Teixeira, C., Gomes, M. S., Gomes, P., Silva, T., & Ferraz, R. (2023). Improving the Antimycobacterial Drug Clofazimine through Formation of Organic Salts by Combination with Fluoroquinolones. International Journal of Molecular Sciences, 24(2), 1402. https://doi.org/10.3390/ijms2402140210.3390/ijms240214021422-0067info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-03-22T01:47:27Zoai:recipp.ipp.pt:10400.22/22536Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T17:45:02.968910Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
title Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
spellingShingle Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
Bento, Clara M.
Antibiotics
GUMBOS
Ionic liquids
Mycobacterium
Organic salts
Repurposing
Rescuing
title_short Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
title_full Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
title_fullStr Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
title_full_unstemmed Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
title_sort Improving the antimycobacterial drug Clofazimine through formation of organic salts by combination with fluoroquinolones
author Bento, Clara M.
author_facet Bento, Clara M.
Silva, Ana Teresa
Mansano, Bruno
Aguiar, Luísa
Teixeira, Cátia
Gomes, Maria Salomé
Gomes, Paula
Silva, Tânia
Ferraz, Ricardo
author_role author
author2 Silva, Ana Teresa
Mansano, Bruno
Aguiar, Luísa
Teixeira, Cátia
Gomes, Maria Salomé
Gomes, Paula
Silva, Tânia
Ferraz, Ricardo
author2_role author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório Científico do Instituto Politécnico do Porto
dc.contributor.author.fl_str_mv Bento, Clara M.
Silva, Ana Teresa
Mansano, Bruno
Aguiar, Luísa
Teixeira, Cátia
Gomes, Maria Salomé
Gomes, Paula
Silva, Tânia
Ferraz, Ricardo
dc.subject.por.fl_str_mv Antibiotics
GUMBOS
Ionic liquids
Mycobacterium
Organic salts
Repurposing
Rescuing
topic Antibiotics
GUMBOS
Ionic liquids
Mycobacterium
Organic salts
Repurposing
Rescuing
description This work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutical ingredients (API-OSs), as those herein disclosed, hold promise as cost-effective formulations with improved features over their parent drugs, thus enabling the mitigation of some of their shortcomings. For instance, in the specific case of clofazimine, its poor solubility severely limits its bioavailability. As compared to clofazimine, the clofazimine-derived OSs now reported have improved solubility and thermostability, without any major deleterious effects on the drug’s bioactivity profile.
publishDate 2023
dc.date.none.fl_str_mv 2023-03-17T17:05:46Z
2023-01-11
2023-01-11T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10400.22/22536
url http://hdl.handle.net/10400.22/22536
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Bento, C. M., Silva, A. T., Mansano, B., Aguiar, L., Teixeira, C., Gomes, M. S., Gomes, P., Silva, T., & Ferraz, R. (2023). Improving the Antimycobacterial Drug Clofazimine through Formation of Organic Salts by Combination with Fluoroquinolones. International Journal of Molecular Sciences, 24(2), 1402. https://doi.org/10.3390/ijms24021402
10.3390/ijms24021402
1422-0067
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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