Objective: The aim of the present study is to synthesize novel benzimidazole derivatives as potent antifungal agents.Methods: 2-chloromethyl-1H-benzimidazole has been synthesized by refluxing o-phenylenediamine with chloroacetic acid in the presence of 5N HCL. Further, N-substituted benzimidazole derivatives containing various heteroamines and aromatic compounds were synthesized. These, finally, prepared derivatives were kept for in vitro antifungal property.Results: A novel series of antifungal agents, containing benzimidazole nucleus as a basic skeleton, has been synthesized.Conclusion: The synthesized novel benzimidazole derivatives exhibit moderate activity (VMSA 1, 2, 8), some compounds showed significant activity (VMSA 6, 9, and 10), and compound VMSA 4 and 5 exhibits maximum activity.