Combinatorial approach toward synthesis of small molecule libraries as bacterial transglycosylase inhibitors?

Organic & Biomolecular Chemistry Pub Date: 2010-03-29 DOI: 10.1039/C000622J

Abstract

The development of iminocyclitol-based small molecule libraries against a bacterial TGase is described. An iminocyclitol was conjugated with a pyrophosphate mimic using either a 1,3-dipolar cycloaddition or reductive amination reaction, which was then condensed with a variety of lipophilic carboxylic acids in an amide bond coupling to generate a desired molecular library. With assistance of microtiter plate-based combinatorial chemistry and in situ screening, a potential inhibitor, the first potent iminocyclitol-based inhibitor against bacterial TGases was efficiently developed.

Graphical abstract: Combinatorial approach toward synthesis of small molecule libraries as bacterial transglycosylase inhibitors
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