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New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents.
Chiarelli, Laurent R; Mori, Matteo; Beretta, Giangiacomo; Gelain, Arianna; Pini, Elena; Sammartino, Josè Camilla; Stelitano, Giovanni; Barlocco, Daniela; Costantino, Luca; Lapillo, Margherita; Poli, Giulio; Caligiuri, Isabella; Rizzolio, Flavio; Bellinzoni, Marco; Tuccinardi, Tiziano; Villa, Stefania; Meneghetti, Fiorella.
Afiliación
  • Chiarelli LR; a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.
  • Mori M; b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.
  • Beretta G; c Department of Environmental Science and Policy , University of Milano , Milano , Italy.
  • Gelain A; b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.
  • Pini E; b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.
  • Sammartino JC; a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.
  • Stelitano G; a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.
  • Barlocco D; b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.
  • Costantino L; d Department of Life Sciences , University of Modena e Reggio Emilia , Modena , Italy.
  • Lapillo M; e Department of Pharmacy , University of Pisa , Pisa , Italy.
  • Poli G; e Department of Pharmacy , University of Pisa , Pisa , Italy.
  • Caligiuri I; f Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano , Italy.
  • Rizzolio F; f Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano , Italy.
  • Bellinzoni M; g Department of Molecular Science and Nanosystems , Ca' Foscari University of Venezia , Venezia-Mestre , Italy.
  • Tuccinardi T; h Institut Pasteur , Paris , France.
  • Villa S; e Department of Pharmacy , University of Pisa , Pisa , Italy.
  • Meneghetti F; b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.
J Enzyme Inhib Med Chem ; 34(1): 823-828, 2019 Dec.
Article en En | MEDLINE | ID: mdl-30889995
ABSTRACT
Starting from the analysis of the hypothetical binding mode of our previous furan-based hit (I), we successfully achieved our objective to replace the nitro moiety, leading to the disclosure of a new lead exhibiting a strong activity against MbtI. Our best candidate 1 h displayed a Ki of 8.8 µM and its antimycobacterial activity (MIC99 = 250 µM) is conceivably related to mycobactin biosynthesis inhibition. These results support the hypothesis that 5-phenylfuran-2-carboxylic derivatives are a promising class of MbtI inhibitors.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Furanos / Liasas / Antituberculosos Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Italia
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Furanos / Liasas / Antituberculosos Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Italia