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

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.