Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 17, Pages 7476-7482Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00834
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Funding
- National Research Foundation (NRF)
- University of KwaZulu-Natal (South Africa)
- International Scientific Partnership Program ISPP at King Saud University (Saudi Arabia) [0061]
- MINECO [CTQ2015-67870-P]
- Generalitat de Catalunya (Spain) [SGR 137]
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Teixobactin is a head to side chain cyclo-depsipeptide 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 SAP. 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.
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