Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis
2020-12-26
| Authors: | ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; |
|---|---|
| Format: | Article |
| Status: | Published version |
| Publication date: | 2009 |
| Country: | Brasil |
| Institution: | FIOCRUZ |
| Repository: | Repositório Institucional da FIOCRUZ (ARCA) |
| Language: | English |
| OAI Identifier: | oai:arca.fiocruz.br:icict/38828 |
| Online Access: | https://arca.fiocruz.br/handle/icict/38828 |
| Access Level: | Open access |
| Keyword: | Tuberculosis Mycobacterium avium Mycobacterium tuberculosis Anti-tuberculosis drugs |
| _version_ | 1878754962724356096 |
|---|---|
| author | Figueiredo, Ricardo |
| author2 | Moiteiro, Cristina Medeiros, M. Augusta Silva, P. Almeida da Ramos, D. Spies, F. Ribeiro, M. O. Lourenço, M. Cristina S. Neves Júnior, I. N. Gaspar, M. Manoela Cruz, M. Eugénia M. Curto, M. João Marcelo Franzblau, S. G. Orozco, H. Aguilar, D. Hernandez-Pando, R. Costa, M. Céu |
| author2_role | author author author author author author author author author author author author author author author author |
| author_browse | Aguilar, D. Costa, M. Céu Cruz, M. Eugénia M. Curto, M. João Marcelo Figueiredo, Ricardo Franzblau, S. G. Gaspar, M. Manoela Hernandez-Pando, R. Lourenço, M. Cristina S. Medeiros, M. Augusta Moiteiro, Cristina Neves Júnior, I. N. Orozco, H. Ramos, D. Ribeiro, M. O. Silva, P. Almeida da Spies, F. |
| author_facet | Figueiredo, Ricardo Moiteiro, Cristina Medeiros, M. Augusta Silva, P. Almeida da Ramos, D. Spies, F. Ribeiro, M. O. Lourenço, M. Cristina S. Neves Júnior, I. N. Gaspar, M. Manoela Cruz, M. Eugénia M. Curto, M. João Marcelo Franzblau, S. G. Orozco, H. Aguilar, D. Hernandez-Pando, R. Costa, M. Céu |
| author_role | author |
| bitstream_url_str_mv | https://arca.fiocruz.br/bitstreams/caa2c7bb-d13f-40f0-b662-9f0acd815bd2/download https://arca.fiocruz.br/bitstreams/60b82327-3130-4fd9-83ce-f264984727fe/download https://arca.fiocruz.br/bitstreams/641bc7b1-bff2-4c4d-8f29-0ac0ca336c00/download https://arca.fiocruz.br/bitstreams/b71da960-923d-4d89-9413-126455b3a253/download |
| collection | Repositório Institucional da FIOCRUZ (ARCA) |
| description | 2020-12-26 |
| eu_rights_str_mv | openAccess |
| format | article |
| id | BR_4c641ffc202ebf2f4b76cb78c5b3b3a8 |
| identifier_str_mv | 10.1016/j.bmc.2008.12.006 |
| institution | FIOCRUZ |
| instname_str | Fundação Oswaldo Cruz (FIOCRUZ) |
| language | eng |
| network_acronym_str | BR |
| network_name_str | Brasil |
| oai_identifier_str | oai:arca.fiocruz.br:icict/38828 |
| publishDate | 2009 |
| publishDateSort | 2009 |
| publisher | Elsevier |
| publisherStr | Elsevier |
| reponame_str | Repositório Institucional da FIOCRUZ (ARCA) |
| spelling | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis Figueiredo, Ricardo Moiteiro, Cristina Medeiros, M. Augusta Silva, P. Almeida da Ramos, D. Spies, F. Ribeiro, M. O. Lourenço, M. Cristina S. Neves Júnior, I. N. Gaspar, M. Manoela Cruz, M. Eugénia M. Curto, M. João Marcelo Franzblau, S. G. Orozco, H. Aguilar, D. Hernandez-Pando, R. Costa, M. Céu Tuberculosis Mycobacterium avium Mycobacterium tuberculosis Anti-tuberculosis drugs 2020-12-26 Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. Universidade Federal do Rio Grande. Rio Grande, RS, Brasil. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brasil. .University of Illinois. Institute for Tuberculosis Research. Chicago, IL, USA. National Institute of Medical Sciences and Nutrition Salvador Zubirán. Mexico, DF, Mexico National Institute of Medical Sciences and Nutrition Salvador Zubirán. Mexico, DF, Mexico. Clinical utility of rifabutin1 (RBT), a potent antibiotic used in multidrug regimens for tuberculosis (TB) aswell as for infections caused by Mycobacterium avium complex (MAC), has been hampered due to dose-limiting toxicity. RBT analogs 2–11 were synthesized and evaluated against M. avium 1581 and Mycobacterium tuberculosis susceptible and resistant strains in vitro. A selection of candidates were also assayed against non-replicating persistent (NRP)M. tuberculosis. Subsequent in vivo studies with the best preclinical candidate drugs 5 and 8, in a model of progressive pulmonary tuberculosis of Balb/C mice infected either with H37Rv drug–sensible strain or with multidrug resistant (MDR) clinical isolates, resistant toall primary antibiotics including rifampicin, were performed. The results disclosed here suggest that 5 and 8 have potential for clinical application. Elsevier FIGUEIREDO, Ricardo et al. Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H37Rv, MDR and NRPMycobacterium tuberculosis. Bioorganic and Medicinal Chemistry, v. 17, p. 503-511, 2009. 0968-0896 https://arca.fiocruz.br/handle/icict/38828 10.1016/j.bmc.2008.12.006 |
| spellingShingle | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis Figueiredo, Ricardo Tuberculosis Mycobacterium avium Mycobacterium tuberculosis Anti-tuberculosis drugs |
| status_str | publishedVersion |
| title | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis |
| title_full | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis |
| title_fullStr | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis |
| title_full_unstemmed | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis |
| title_short | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis |
| title_sort | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis |
| topic | Tuberculosis Mycobacterium avium Mycobacterium tuberculosis Anti-tuberculosis drugs |
| topic_facet | Tuberculosis Mycobacterium avium Mycobacterium tuberculosis Anti-tuberculosis drugs |
| url | https://arca.fiocruz.br/handle/icict/38828 |