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Updated: Dec 18, 2025

Gramicidin-based Fluorescence Assay; for Determining Small Molecules Potential for Modifying Lipid Bilayer Properties
Published on: October 13, 2010
Synthesis and biological evaluation of backbone-aminated analogues of gramicidin S
Benjamin M Rathman1, Jessie L Allen2, Lindsey N Shaw2
1Department of Chemistry & Biochemistry, University of Notre Dame, Notre Dame, IN 46556, United States.
Abstract:
We report the parallel synthesis of gramicidin S derivatives featuring backbone N-amino substituents. Analogues were prepared by incorporation of N-amino dipeptide subunits on solid support. Nine backbone-aminated macrocycles were evaluated for growth inhibitory activity against ESKAPE pathogens and hemolytic activity against human red blood cells. Diamination of the Orn residues in the β-strand region of gramicidin S was found to enhance broad-spectrum antimicrobial activity without a corresponding increase in hemolytic activity.
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