Fungal infections are increasing rapidly due to an increase in number of immuno-compromised hosts. Azoles are first line drugs for treatment of fungal infections due to their high therapeutic index but development of resistance due to extensive use of azoles and toxicity has significantly reduced the efficacy of azole antifungal agents and led to the search for new azoles. Azoles act by competitive inhibition of cytochrome P 450 (CYP450) enzyme, Lanosterol 14α-demethylase a key enzyme in biosynthesis of sterol in fungi. From the study of active site of the enzyme and SAR of azole antifungal agents, benzyl benzimidazole derivatives were designed and synthesized. The structures of the synthesized compounds were elucidated by spectral data. The synthesized compounds were screened for antifungal activity against Candida species by serial dilution method using ketoconazole as a reference standard. Among the synthesized compounds, compounds having polar side chains were found to posses significant antifungal activity.