In a wide search program for new and efficient antimicrobial agents, a series of t(3)-isopropyl-r(2),r(6)-di-2¢-furanylpiperidin-4-one 1 and its derivatives 2–7 were synthesized; characterized by IR, 1 H NMR, 1 H-1 H COSY, 13C NMR, and mass and elemental analysis; and their antibacterial activity against Streptococcus faecalis, Bacillus subtilis, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa and antifungal activity against Candida-6, Candida albicans, Aspergillus niger, Candida-51 and Aspergillus flavus was evaluated. Compound 6 exerted potent in vitro antibacterial activity against B. subtilis while compound 6 exhibited in vitro antifungal activity against Candida-6.