Antimicrobial activities of chemically modified thiazolyl peptide antibiotic MDL 62,879 (GE2270A).
Open Access
- 1 January 1997
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 50 (4) , 344-349
- https://doi.org/10.7164/antibiotics.50.344
Abstract
MDL 62, 879 (GE2270A) 1 is a new inhibitor of elongation factor-Tu (EF-Tu) and belongs to the class of thiazolyl pep tide antibiotics. Controlled acid hydrolysis of 1 followed by treatment with base resulted in the lost of the two terminal amino acids and in the formation of water-soluble MDL 62, 935 2. Although less active in vitro than its parent compound, 2 was able to inhibit by 50% an Escherichia coli cell-free protein synthesis system at roughly the same concentration of 1. MDL 62, 935 2 was subjected to further modification at the β-phenylserine residue. Derivatives obtained from 2 were less active in both antimicrobial (MIC) and enzymatic (IC50) assays. This suggests that β-phenylserine plays an important role for the inhibition of EF-Tu by 1 and 2.Keywords
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