A　series　of　novel　benzofuran-isatin-hydroxylimine/thiosemicarbazide　hybrids　were　designed,　synthesized　and　evaluated　for　their　in　vitro　anti-TB　activities　against　drug-sensitive　MTB　H(37)Rv　and　MDR-TB　isolates　as　well　as　cytotoxicity.　All　benzofuran-isatin-hydroxylimine/thiosemicarbazide　hybrids　exhibited　considerable　in　vitro　anti-mycobacterial　activities　against　the　tested　three　MTB　strains,　and　all　of　them　also　showed　acceptable　cytotoxicity.　The　most　active　hybrid　7f　was　＞4.8　and　＞51　folds　more　potent　than　the　first　line　anti-TB　agents　RIF　and　INH　against　both　drug-sensitive　MTB　H(37)Rv　and　MDR-TB　isolates,　respectively.　The　results　demonstrated　the　potential　utility　of　benzofuran-isatin-hydroxylimine/-thiosemicarbazide　hybrids　as　anti-TB　agents.　(C)　2018　Chinese　Chemical　Society　and　Institute　of　Materia　Medica,　Chinese　Academy　of　Medical　Sciences.　Published　by　Elsevier　B.V.　All　rights　reserved.