Combretum zeyheri Sond (Combretaceae) has been reported to exhibit anticandida activity against Candida kruzei, C. albicans, and C. parapsilosis; however, the active constituents have not been isolated so far. A bioactivity-guided fractionation of MeOH extract of C. zeyheri resulted in the isolation of triterpenoids, ursolic acid (1.1), oleanolic acid (1.2), maslinic acid (2.1), 2a,3b-dihydroxyurs-12-en-28-oic acid (2.2), 6b-hydroxymaslinic acid (3), and terminolic acid (4). These compounds were characterized on the basis of their 1D, 2D NMR, ESI-MS and FT-IR spectroscopic data. All the isolated compounds, 1.2, 2.1, 2.2, 3, and 4 except ursolic acid (1.1) are being reported for the first time from C. zeyheri. Later, the isolated triterpenoids (1–4) were evaluated for their anticandida activity against the three strains of C. albicans and all compounds showed anticandida activity of which terminolic acid (4) was most active. Furthermore, structure– activity relationship of isolated triterpenoids (1–4) was studied, which showed that triterpenoids of oleanane and ursane having 2a,3b,23-trihydroxyl group are more active.