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Alkyl-guanidine Compounds as Potent Broad-Spectrum Antibacterial Agents: Chemical Library Extension and Biological Characterization.
Pasero, Carolina; D'Agostino, Ilaria; De Luca, Filomena; Zamperini, Claudio; Deodato, Davide; Truglio, Giuseppina I; Sannio, Filomena; Del Prete, Rosita; Ferraro, Teresa; Visaggio, Daniela; Mancini, Arianna; Guglielmi, Mario B; Visca, Paolo; Docquier, Jean-Denis; Botta, Maurizio.
Afiliación
  • Pasero C; Department of Biotechnology, Chemistry, and Pharmacy , University of Siena , I-53100 Siena , Italy.
  • D'Agostino I; Department of Biotechnology, Chemistry, and Pharmacy , University of Siena , I-53100 Siena , Italy.
  • De Luca F; Department of Medical Biotechnology , University of Siena , I-53100 Siena , Italy.
  • Zamperini C; Department of Biotechnology, Chemistry, and Pharmacy , University of Siena , I-53100 Siena , Italy.
  • Deodato D; Lead Discovery Siena s.r.l. , Via Vittorio Alfieri 31 , I-53019 Castelnuovo Berardenga , Italy.
  • Truglio GI; Department of Biotechnology, Chemistry, and Pharmacy , University of Siena , I-53100 Siena , Italy.
  • Sannio F; Department of Biotechnology, Chemistry, and Pharmacy , University of Siena , I-53100 Siena , Italy.
  • Del Prete R; Department of Medical Biotechnology , University of Siena , I-53100 Siena , Italy.
  • Ferraro T; Department of Medical Biotechnology , University of Siena , I-53100 Siena , Italy.
  • Visaggio D; Lead Discovery Siena s.r.l. , Via Vittorio Alfieri 31 , I-53019 Castelnuovo Berardenga , Italy.
  • Mancini A; Department of Sciences , Roma Tre University , Rome 00146 , Italy.
  • Guglielmi MB; Department of Biotechnology, Chemistry, and Pharmacy , University of Siena , I-53100 Siena , Italy.
  • Visca P; Biogem, Research Institute , Ariano Irpino , AV Italy.
  • Docquier JD; Department of Sciences , Roma Tre University , Rome 00146 , Italy.
  • Botta M; Department of Medical Biotechnology , University of Siena , I-53100 Siena , Italy.
J Med Chem ; 61(20): 9162-9176, 2018 10 25.
Article en En | MEDLINE | ID: mdl-30265809
Nowadays, the increasing of multidrug-resistant pathogenic bacteria represents a serious threat to public health, and the lack of new antibiotics is becoming a global emergency. Therefore, research in antibacterial fields is urgently needed to expand the currently available arsenal of drugs. We have recently reported an alkyl-guanidine derivative (2), characterized by a symmetrical dimeric structure, as a good candidate for further developments, with a high antibacterial activity against both Gram-positive and Gram-negative strains. In this study, starting from its chemical scaffold, we synthesized a small library of analogues. Moreover, biological and in vitro pharmacokinetic characterizations were conducted on some selected derivatives, revealing notable properties: broad-spectrum profile, activity against resistant clinical isolates, and appreciable aqueous solubility. Interestingly, 2 seems neither to select for resistant strains nor to macroscopically alter the membranes, but further studies are required to determine the mode of action.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Guanidina / Antibacterianos Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Guanidina / Antibacterianos Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos