Synthesis and Structure-Activity Relationships of α-Amino-γ-lactone Ketolides: A Novel Class of Macrolide Antibiotics.

Abstract

An efficient synthesis of α-amino-γ-lactone ketolide (3) was developed, which provided a versatile intermediate for the incorporation of a variety of aryl and heteroaryl groups onto the C-21 position of clarithromycin via HBTU-mediated amidation. The biological data for this important new class of macrolides revealed significantly potent activity against… (More)
DOI: 10.1021/ml500279k

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Cite this paper

@article{Pavlovi2014SynthesisAS, title={Synthesis and Structure-Activity Relationships of α-Amino-γ-lactone Ketolides: A Novel Class of Macrolide Antibiotics.}, author={Dra{\vz}en Pavlovi{\'c} and Stjepan Mutak and D. Andreotti and Stefano Biondi and Francesca Cardullo and Alfredo Paio and Elisa Piga and Daniele Donati and Sergio Lociuro}, journal={ACS medicinal chemistry letters}, year={2014}, volume={5 10}, pages={1133-7} }