| Author | Figueiredo, Ricardo | |
| Author | Moiteiro, Cristina | |
| Author | Medeiros, M. Augusta | |
| Author | Silva, P. Almeida da | |
| Author | Ramos, D. | |
| Author | Spies, F. | |
| Author | Ribeiro, M. O. | |
| Author | Lourenço, M. Cristina S. | |
| Author | Neves Júnior, I. N. | |
| Author | Gaspar, M. Manoela | |
| Author | Cruz, M. Eugénia M. | |
| Author | Curto, M. João Marcelo | |
| Author | Franzblau, S. G. | |
| Author | Orozco, H. | |
| Author | Aguilar, D. | |
| Author | Hernandez-Pando, R. | |
| Author | Costa, M. Céu | |
| Access date | 2019-12-26T13:16:23Z | |
| Available date | 2019-12-26T13:16:23Z | |
| Document date | 2009 | |
| Citation | 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. | pt_BR |
| ISSN | 0968-0896 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/38828 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | open access | pt_BR |
| Title | Synthesis and evaluation of rifabutin analogs against Mycobacteium avium and H(37) Rv, MDR and NRP Mycobacterium tuberculosis | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.1016/j.bmc.2008.12.006 | |
| Abstract | 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. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Affilliation | Universidade Federal do Rio Grande. Rio Grande, RS, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Rio Grande. Rio Grande, RS, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Rio Grande. Rio Grande, RS, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Rio Grande. Rio Grande, RS, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Affilliation | .University of Illinois. Institute for Tuberculosis Research. Chicago, IL, USA. | pt_BR |
| Affilliation | National Institute of Medical Sciences and Nutrition Salvador Zubirán. Mexico, DF, Mexico | pt_BR |
| Affilliation | National Institute of Medical Sciences and Nutrition Salvador Zubirán. Mexico, DF, Mexico | pt_BR |
| Affilliation | National Institute of Medical Sciences and Nutrition Salvador Zubirán. Mexico, DF, Mexico. | pt_BR |
| Affilliation | Instituto Nacional de Engenharia, Tecnologia e Inovação. Lisboa, Portugal. | pt_BR |
| Subject | Tuberculosis | pt_BR |
| Subject | Mycobacterium avium | pt_BR |
| Subject | Mycobacterium tuberculosis | pt_BR |
| Subject | Anti-tuberculosis drugs | pt_BR |
| Embargo date | 2020-12-26 | |
