Teicoplanin antibacterial activity

Other specific discovery assays have been used such as differential inhibition of a vancomycin resistant S. aureus strain and its susceptible parent, and an assay based on antagonism of the antibacterial activity by N,A/-diacetyl-L-Lys-D-Ala-D-Ala [24570-39-6] a tripeptide analogue of the dalbaheptides receptor. AppHcation of this latter test to 1936 cultures (90) led to the isolation of 42 dalbaheptides, six of which, including kibdelin (Table 3), parvodicin (Table 3), and actinoidin A2 (68) were novel. A colorimetric assay based on competition between horseradish peroxidase bound teicoplanin and the... 

NJ Snyder, RD Cooper, BS Briggs, M Zmijewski, DL Mullen, RE Kaiser, TI Nicas. Enzymatic deacylation of teicoplanin followed by reductive alkylation synthesis and antibacterial activity of new glycopeptides. J Antibiot 51 945-951, 1998. 

Campoli-Richards DM, Brogden RN, Faulds D. Teicoplanin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic potential. Drugs 1990 40(3) 449-86. 

The C-terminal residues of 46 both possess d stereochemistry, and stimulated the design of peptide 93, which retains a turn-promoting moiety, and replaces the C-terminal residues with the o-Ala-o-Ala motif. This new catalyst allowed for the efficient conversion of 89 to diphenylphosphate 92 in 41 % isolated yield. Following deprotection of 90-92, each phosphorylated analog showed attenuated activity toward most of the tested in antibacterial assays, providing some SAR information for the teicoplanin hydroxyl array [153, 154]. 

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