BACKGROUNDCrataegus orientalis Pall. ex M. Bieb fruit (COPMB) is extensively used as a source of various products in the medicinal‐aromatic field and holds the potential for erosion control, ornamental purposes, food source, and economic benefits for forest villagers from its fruits. This study aims to determine the chemical components and biological activities of extracts prepared from COPMB using different solvents.RESULTSThe present work was designed to define the antioxidant activity [phosphomolybdenum (total antioxidant capacity), 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric ion‐reducing antioxidant capacity (CUPRAC) and metal chelating activity (MCA)], phytochemical screening analysis, enzyme inhibitor (α‐amylase, α‐glucosidase and tyrosinase) potential, and liquid chromatography‐high resolution mass spectrometry (LC‐HRMS) secondary metabolite profiling in different extracts of COPMB. The results of LC‐HRMS revealed that fumaric acid was the main phenolic compound in all extracts. Among the extracts, ethyl acetate extract has the highest phytochemical and antioxidant properties [total phenolic content (TPC): 32.5 mg GAE/g, total flavonoid content (TFC): 12.2 mg QE/g, ABTS: 213.0 mg TE/g; CUPRAC: 126.0 mg TE/g, MCA: 145.0 mg EDTA/g; FRAP: 122.8 mg TE/g; TAC: 2.8 mmol TE/g]. Ethyl acetate and methanol extracts are more effective in α‐amylase (0.27 ± 0.01 mg/mL; 0.12 ± 0.00 mg/mL), α‐glucosidase (0.63 ± 0.02 mg/mL; 0.77 ± 0.02 mg/mL) and tyrosinase (0.03 ± 0.00 mg/mL; 0.03 ± 0.00 mg/mL) enzyme inhibition potentials compared to standard acarbose (0.75 ± 0.02 mg/mL for α‐amylase; 1.11 ± 0.03 mg/mL for α‐glucosidase) and kojic acid (0.04 ± 0.00 mg/mL).CONCLUSIONThe findings from this study suggest that COPMB could serve as a valuable source of natural agents for the food and pharmaceutical industry. © 2024 Society of Chemical Industry.