Stevioside and steviolbioside, glycosides from Stevia rebaudiana Bertoni, in addition to hybrid compounds synthesized from steviolbioside and the antituberculosis drug isoniazid and its isomer nicotinic acid hydrazide exhibited moderate antituberculosis activity against M. tuberculosis strain H37RV in vitro (MIC = 7.5, 3.75,5, and 10 g/mL, respectively).