Phytochemical studies on the methanolic extract of Drypetes gossweileri afforded N-b-D-glucopyranosylp-hydroxyphenylacetamide (1), p-hydroxyphenylacetic acid (2), p-hydroxyphenyl-acetonitrile (3), phydroxyacetophenone (4), 3,4,5-trimethoxyphenol (5), dolichandroside A (6), and b-amyrone (7). Compounds 1–7 were identified with the aid of extensive NMR and MS spectroscopic studies. Compound 1 was a new natural product and was isolated for the first time from plant containing N-glucose moiety incorporated in its structure. Compounds 1–7 exhibited moderate to the weak source anti-a-glucosidase inhibitory activity. Compound 7 exhibited moderate anti-acetylcholinesterase (AChE) activity while the rest of the isolates were weakly active in this bioassay. Compounds 1–7 also showed moderate antifungal activity.