Modifying Heterocycles to Treat Gram Positive and Gram Negative Bacteria

Abstract

Bacterial infections are a serious threat to human health. During the award period we focused on the synthesis of some phenazines with potential antimicrobial activity. Our hypothesis is the conjugation of amines, polyamines and peptides to the phenazines will enhance their activity. We achieve the synthesis of several new phenazines containing diverse functional groups. Most of the new compounds presented modest antibacterial activity, thus, a structural optimization is being performed using the obtained data. The attachment of amines to the active phenazines proved difficult due to a rearrangement that took places. Thus, we focused in optimizing the structure of potential peptides that can be added to the phenazines. We prepared and evaluated some intriguing new peptides that presented potent activity against a panel of gram positive and gram negative pathogens. We also identified some key features that give rise to their activity. Over the next year we will focus on creating phenazine-peptide conjugates as novel antibacterials.

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Document Details

Document Type
Technical Report
Publication Date
May 01, 2019
Accession Number
AD1093916

Entities

People

  • Martin Conda-Sheridan

Organizations

  • University of Nebraska Medical Center

Tags

DTIC Thesaurus Topics

  • Amines
  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Bacteria
  • Bacterial Infections
  • Bacteriology
  • Biomedical Research
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Escherichia Coli
  • Health Services
  • Medical Personnel
  • Microbiology
  • Organic Chemistry
  • Three Dimensional

Readers

  • Electrochemical Engineering/ Fuel Cell Technologies
  • Molecular and Cellular Biochemistry
  • Systems Analysis and Design