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Structure-Function Studies on IMD-0354 Identifies Highly Active Colistin Adjuvants.
Nemeth, Ansley M; Basak, Akash K; Weig, Alexander W; Marrujo, Santiana A; Barker, William T; Jania, Leigh A; Hendricks, Tyler A; Sullivan, Ashley E; O'Connor, Patrick M; Melander, Roberta J; Koller, Beverly H; Melander, Christian.
Afiliación
  • Nemeth AM; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Basak AK; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Weig AW; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Marrujo SA; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Barker WT; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Jania LA; Department of Genetics, University of North Carolina at Chapel Hill, Chapel Hill, NC 2759, USA.
  • Hendricks TA; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Sullivan AE; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • O'Connor PM; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Melander RJ; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
  • Koller BH; Department of Genetics, University of North Carolina at Chapel Hill, Chapel Hill, NC 2759, USA.
  • Melander C; Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
ChemMedChem ; 15(2): 210-218, 2020 01 17.
Article en En | MEDLINE | ID: mdl-31756025
Infections caused by multidrug-resistant (MDR) bacteria, particularly Gram-negative bacteria, are an escalating global health threat. Often clinicians are forced to administer the last-resort antibiotic colistin; however, colistin resistance is becoming increasingly prevalent, giving rise to the potential for a situation in which there are no treatment options for MDR Gram-negative infections. The development of adjuvants that circumvent bacterial resistance mechanisms is a promising orthogonal approach to the development of new antibiotics. We recently disclosed that the known IKK-ß inhibitor IMD-0354 potently suppresses colistin resistance in several Gram-negative strains. In this study, we explore the structure-activity relationship (SAR) between the IMD-0354 scaffold and colistin resistance suppression, and identify several compounds with more potent activity than the parent against highly colistin-resistant strains of Acinetobacter baumannii and Klebsiella pneumoniae.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzamidas / Adyuvantes Farmacéuticos / Acinetobacter baumannii / Klebsiella pneumoniae / Antibacterianos Límite: Humans Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Alemania

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzamidas / Adyuvantes Farmacéuticos / Acinetobacter baumannii / Klebsiella pneumoniae / Antibacterianos Límite: Humans Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Alemania