In the present communication, a series based on 1-[2-(6-nitro-4-oxo-2-phenyl-4H-quinazolin-3-yl)-ethyl]- 3-phenyl-urea have been synthesized by an efficient synthetic protocol. The synthesized compounds were characterized by IR, 1 H NMR, 13C NMR spectroscopy, ESI Mass spectrometry, and elemental analysis. The antibacterial and antifungal activity of the compounds were studied against selected strains (Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Bacillus subtilis ATCC 11774, and Candida albicans ATCC 66027) by using Kirby Bauer disk diffusion technique and broth dilution technique. All the synthesized compounds showed good antifungal potency against strain C. albicans.