The present study describes designing of Polycarponin B and its N-methylated analog by retrosynthetic analysis. Synthesis of the titled compounds was then carried out by solution phase technique. The structure of the synthesized compounds was confirmed by IR, 1H NMR, 13C NMR, Mass and elemental analysis. The compounds were evaluated for antimicrobial, antifungal and antioxidant activity. From the results of biological activity it was concluded that newly synthesized compound possessed very good activity against Gram positive bacteria and moderate activity against Gram negative bacteria and pathogenic fungi. The N-methylated analog of Polycarponin B showed increase in the antimicrobial and antioxidant activity in comparison with Polycarponin B.