Journal of Medicinal Chemistry
Journal of Medicinal Chemistry
5 years ago

Converting Teixobactin into a Cationic Antimicrobial Peptide (AMP)

Converting Teixobactin into a Cationic Antimicrobial Peptide (AMP)
Beatriz G. de la Torre, Estelle J. Ramchuran, Shimaa A. H. Abdel Monaim, Fernando Albericio, Ayman El-Faham
Teixobactin is a head to side chain cyclodepsipeptide that contains two positive charges. One is found in the cycle, as a result of the presence of the guanidino-unusual amino acid L-allo-End, while the other is at the N-terminal. Here we introduce 26 new Teixobactin analogues with an increasing number of positive charges. In an attempt to fine-tune the biological activity of Teixobactin, we examined the effect of cationicity on the SAR of these analogues. The maximum number of positive charges to maintain the activity are three to four. Analogues with five positive charges show the lowest activity.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00834

DOI: 10.1021/acs.jmedchem.7b00834

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