Synthesis and antibacterial evaluation of some teicoplanin pseudoaglycon derivatives containing alkyl- and arylthiosubstituted maleimides

Magdolna Csávás; Adrienn Miskovics; Zsolt Szűcs; Erzsébet Rőth; Zsolt L Nagy; Ilona Bereczki; Mihály Herczeg; Gyula Batta; Éva Nemes-Nikodém; Eszter Ostorházi; Ferenc Rozgonyi; Anikó Borbás; Pál Herczegh

doi:10.1038/ja.2015.33

Synthesis and antibacterial evaluation of some teicoplanin pseudoaglycon derivatives containing alkyl- and arylthiosubstituted maleimides

J Antibiot (Tokyo). 2015 Sep;68(9):579-85. doi: 10.1038/ja.2015.33. Epub 2015 Apr 1.

Affiliations

¹ Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
² Department of Organic Chemistry, University of Debrecen, Debrecen, Hungary.
³ Department of Dermatology, Venerology and Dermatooncology, Microbiology Laboratory, Semmelweis University, Budapest, Hungary.

PMID: 25829202
DOI: 10.1038/ja.2015.33

Abstract

Bis-alkylthio maleimido derivatives have been prepared from teicoplanin pseudoaglycon by reaction of its primary amino group with N-ethoxycarbonyl bis-alkylthiomaleimides. Some of the new derivatives displayed excellent antibacterial activity against resistant bacteria.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Bacteria / drug effects*
Drug Resistance, Bacterial
Maleimides / chemical synthesis
Maleimides / chemistry
Maleimides / pharmacology*
Teicoplanin / chemical synthesis
Teicoplanin / chemistry
Teicoplanin / pharmacology*

Substances

Anti-Bacterial Agents
Maleimides
Teicoplanin