Bioassay-guided fractionation of the active AcOEt-soluble layer from the whole plant of Amischotolype hispida resulted in the isolation of four new compounds, i.e., amisbenzoic acid (1), one butenolide derivative, amisnolide (2), one chlorin analog, amisphytin (3), one lignan, amislignol (4), and one metabolite isolated for the first time from nature, (À)-glaberide I (5), along with 20 known compounds, 6 -25. Their structures were elucidated on the basis of UV, IR, 1D-and 2D-NMR ( 1 H, 1 H-COSY, DEPT, HSQC, HMBC), as well as HR-ESI-MS, analyses. Among these isolates, palmitic acid (13) showed an antimycobacterial activity with an MIC value of 20.0 mg/ml against Mycobacterium tuberculosis H37Rv.