Eremomycin pyrrolidide: a novel semisynthetic glycopeptide with improved chemotherapeutic properties

Drug Design, Development and Therapy
Evgenia N OlsufyevaMaria N Preobrazhenskaya

Abstract

Development of new semisynthetic glycopeptides with improved antibacterial efficacy and reduced pseudoallergic reactions. Semisynthetic glycopeptides 3-6 were synthesized from vancomycin (1) or eremomycin (2) by the condensation with pyrrolidine or piperidine. The minimum inhibitory concentration (MIC) for the new derivatives was measured by the broth micro-dilution method on a panel of clinical isolates of Staphylococcus and Enterococcus. Acute toxicity (50% lethal dose, maximum tolerated doses), antibacterial efficacy on model of systemic bacterial infection with S. aureus and pseudoallergic inflammatory reaction (on concanavalin A) of eremomycin pyrrolidide (5) were evaluated in mice according to standard procedures. The eremomycin pyrrolidide (5) was the most active compound and showed a high activity against Gram-positive bacteria: vancomycin-susceptible staphylococci and enterococci (minimum inhibitory concentrations [MICs] 0.13-0.25 mg/L), as well as vancomycin-intermediate resistant Staphylococcus aureus (MICs 1 mg/L). Antimicrobial susceptibility tested on a panel of 676 isolates showed that 5 had similar activity for the genera Staphylococcus and Enterococcus with MIC90=0.5 mg/L, while vancomycin had MIC90=1-2 mg/L. T...Continue Reading

Citations

Dec 29, 2020·Journal of Chromatography. a·Dmitry V YaroshenkoAlla V Chernobrovkina
May 1, 2021·Pharmaceuticals·Elena I MoiseenkoAndrey E Shchekotikhin

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Methods Mentioned

BETA
nuclear magnetic resonance
column chromatography
amidation

Software Mentioned

OMNIC
StatPlus
AnalystSoft

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