A series of novel dihydropyrimidin-2(1H)-ones derivatives is synthesized by using Rhizopus Oryzae lipase biocatalyst in deep eutectic solvent. The reaction is characterized by high efficiency and selectivity, short reaction time, mild and environmentally friendly reaction conditions. The yields are found to be significantly higher and reuse of both the lipase and deep eutectic solvent is possible up to four consecutive cycles. The products are found to exhibit appreciable in vitro antibacterial activity against Echerichia coli, Pseudomonas neumoniae and in vitro antifungal activity against Aspergillus niger and Candida albicans.