The need to scientifically proof the traditional claim of the medicinal uses of plant materials in combating diseases has led to investigations into the medicinal potencies of some plants. Zanthoxylum zanthoxyloides stem has been traditionally used to treat diabetes, dental, malarial and other pathogenic infections. Ethnobotanical investigations have suggested that Z. zanthoxyloides possesses active phytochemical constituents which are responsible for its observed bioactivity. In this study we attempted to identify and characterize the active compounds in the leaf of the plant, using GC-MS analysis. The methanolic extract of the plant’s leaf was partitioned, and GC-MS analysis was done on the crude alkaloid fraction. The main compounds identified were 2-pentanone 4-hydroxyl-4-methyl (32.96 %), 2-acetoxyisobutyryl chloride (32.96 %), α-hydroxyisobutyric acid acetate (32.96 %). These compounds have been shown to possess antimicrobial, antifungal, antibacterial, antioxidant and hypocholesterolemic properties respectively. The presence of these compounds in the plant corroborates its use in the traditional treatment of several pathogenic and metabolic diseases.