Some series of arylidene barbiturates and thiobarbiturates were evaluated for their antibacterial, antioxidant, and urease inhibition activities. The arylidene barbiturates and thiobarbiturates were tested for antimicrobial activity using the agar well diffusion technique against 13 bacteria. The synthesized compounds (1a–g) were screened for antiurease and antioxidant activities. The results showed that the synthesized compounds (1a–g) had effective antiurease, antioxidant, and antibacterial activities.