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Activity of Rifabutin and Hemi-synthetic Derivatives Against Mycobacterium abscessus.
Ramis, Ivy B; Figueiredo, Ricardo; Ramos, Daniela F; Halicki, Priscila C B; von Groll, Andrea; Viveiros, Miguel; do Ceu Costa, Maria; da Silva, Pedro E A.
Afiliação
  • Ramis IB; Nucleo de Pesquisa em Microbiologia Medica (NUPEMM), Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
  • Figueiredo R; CIPAN, Companhia Industrial Produtora de Antibioticos, Castanheira do Ribatejo, Portugal.
  • Ramos DF; Nucleo de Pesquisa em Microbiologia Medica (NUPEMM), Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
  • Halicki PCB; Nucleo de Pesquisa em Microbiologia Medica (NUPEMM), Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
  • von Groll A; Nucleo de Pesquisa em Microbiologia Medica (NUPEMM), Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
  • Viveiros M; Grupo de Micobacterias, Unidade de Microbiologia Medica, Instituto de Higiene e Medicina Tropical, Universidade Nova de Lisboa, Lisboa, Portugal.
  • do Ceu Costa M; NICiTeS, Escola Superior de Saúde Ribeiro Sanches, Rua do Telhal aos Olivais, n8 - 8a, 1950-396 Lisboa Portugal.
  • da Silva PEA; CBIOS, Escola de Ciencias e Tecnologias da Saude, Universidade Lusofona, Campo Grande, 376, 1749-024 Lisboa, Portugal.
Med Chem ; 14(4): 394-399, 2018.
Article em En | MEDLINE | ID: mdl-29205119
BACKGROUND: Mycobacterium abscessus causes a wide range of clinical diseases that are difficult to treat. This microorganism is resistant not only to the classical antituberculosis agents but also to most of the antimicrobials that are currently available, resulting in limited therapeutic options and treatment failure. This scenario stresses the need to search for new drugs with activity against M. abscessus. OBJECTIVE: To evaluate in vitro the antimycobacterial activity and cytotoxicity of rifabutin (RFB 1) and ten derivatives (2-11) against M. abscessus ATCC 19977. METHOD: The minimum inhibitory concentration (MIC) of the molecules was determined by the microdilution broth method according to the guideline described in CLSI. The toxicity evaluation was carried in 96-well microplates, using the cell line J774A.1 (ATCC TIB-67). RESULT: From the eleven molecules tested, RFB 1 and RFB 4 were the compounds showing higher activities against M. abscessus, with MICs of 0.9 and 1.0 µM, respectively. The R1 and R2 moieties seem to have deciding influence over the final activity. Furthermore, N-oxide derivatives 9, 10, and 11 were also active against M. abscessus, with MICs of 7.2 µM, 1.8 µM and 3.8 µM, respectively. An explanatory hypothesis for the better activities of compounds RFB 1, RFB 4, RFB 10 and RFB 11 considers the likely hydrogen bonding between ligands and receptor, balancing the global flexibility and interaction energies. RFB 1 and its most effective derivatives were found to be not toxic. CONCLUSION: Besides RFB 1, its derivatives 4, 10 and 11 show potential for clinical development in the M. abscessus treatment.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Rifabutina / Antibacterianos Tipo de estudo: Guideline Limite: Animals Idioma: En Revista: Med Chem Assunto da revista: QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Rifabutina / Antibacterianos Tipo de estudo: Guideline Limite: Animals Idioma: En Revista: Med Chem Assunto da revista: QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda