Synthesis of novel pleuromutilin derivatives. Part 1: preliminary studies of antituberculosis activity

Bioorganic & Medicinal Chemistry Letters
Ying-Jie DongZhi-Bin Xu

Abstract

The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20μM, with a MIC of one of the analogues as low as 7.2μM.

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Citations

Nov 30, 2016·Phytotherapy Research : PTR·Marcus Vinícius Oliveira Barros de AlencarMd Torequl Islam
Jul 29, 2016·Natural Product Reports·James R Hanson
Jun 27, 2017·Frontiers in Microbiology·Kate M J de Mattos-ShipleyAndy M Bailey
Aug 27, 2018·Bioorganic & Medicinal Chemistry·Maddie R LemieuxMichio Kurosu

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