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Development of Novel Bacterial Topoisomerase Inhibitors Assisted by Computational Screening.
Powell, Joshua W; Mann, Chelsea A; Toth, Paul D; Nolan, Sheri; Steinert, Anja; Ove, Clarissa; Seffernick, Justin T; Wozniak, Daniel J; Kebriaei, Razieh; Lindert, Steffen; Osheroff, Neil; Yalowich, Jack C; Mitton-Fry, Mark J.
Afiliación
  • Powell JW; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Mann CA; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Toth PD; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Nolan S; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Steinert A; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Ove C; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Seffernick JT; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Wozniak DJ; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Kebriaei R; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Lindert S; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Osheroff N; Division of Medicinal Chemistry and Pharmacognosy, Department of Chemistry and Biochemistry, Microbial Infection and Immunity, Division of Outcomes and Translational Sciences, Department of Microbiology, and Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, Ohio 43210,
  • Yalowich JC; Department of Biochemistry and Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.
  • Mitton-Fry MJ; Department of Biochemistry and Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.
ACS Med Chem Lett ; 15(8): 1287-1297, 2024 Aug 08.
Article en En | MEDLINE | ID: mdl-39140037
ABSTRACT
Multidrug-resistant bacterial infections pose an ever-evolving threat to public health. Since the outset of the antibacterial age, bacteria have developed a multitude of diverse resistance mechanisms that suppress the effectiveness of current therapies. New drug entities, such as Novel Bacterial Topoisomerase Inhibitors (NBTIs), can circumvent this major issue. A computational docking model was employed to predict the binding to DNA gyrase of atypical NBTIs with novel pharmacophores. Synthesis of NBTIs based on computational docking and subsequent antibacterial evaluation against both Gram-positive and Gram-negative bacteria yielded congeners with outstanding anti-staphylococcal activity and varying activity against select Gram-negative pathogens.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2024 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2024 Tipo del documento: Article Pais de publicación: Estados Unidos