Synthesis of novel pleuromutilin derivatives. Part 1: preliminary studies of antituberculosis activity.
Dong YJ, Meng ZH, Mi YQ, Zhang C, Cui ZH, Wang P, Xu ZB.
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.