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Published on: July 20, 2016
Synthesis and characterization of peptide-cationic steroid antibiotic conjugates
Bangwei Ding1, Uale Taotofa, Thomas Orsak
1Department of Chemistry and Biochemistry, Brigham Young University, Provo, Utah 84602, USA.
Abstract:
[reaction: see text] New cationic steroid antibiotics have been prepared by conjugating tripeptides to a triamino analogue of cholic acid. These compounds were synthesized on a solid phase in an indexed library that was screened for antibacterial activity against Gram-negative and Gram-positive bacteria. Selected compounds were synthesized on a larger scale, and minimum inhibition concentrations were measured. These results correlated very well with the screening of the indexed library of antibiotics. The most active antibiotics demonstrate a marked improvement over a related and well characterized cationic steroid antibiotic.
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