Total synthesis and structure-activity relationship of cyclic peptide antibiotic teixobactin:research advances / 国际药学研究杂志
Journal of International Pharmaceutical Research
;
(6): 582-587, 2018.
Article
in Chinese
| WPRIM
| ID: wpr-743042
ABSTRACT
Teixobactin, a cyclic-peptide antibiotic, destroys the cell walls of Gram-positive bacteria. It is therefore difficult for bacteria such as meticillin-resistant Staphylococcus aureus to develop resistance to it. Many scholars have studied the structure-activity relationship (SAR) of teixobactin. After reviewing the reports related to the discovery, structure, total synthesis and SAR of teixobactin, we found that the total synthesis of teixobactin was very difficult. The N-terminal methyl modification, ester bond and allo-End were unnecessary for the activity, the configuration of amino acids at the positions 1, 4, 5 and 8 could greatly influence the antibacterial activity, and the substitution of the amino acids at the 3, 4, 9 and 10 positions by Lys could retain the antibacterial activity.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2018
Type:
Article
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