The present study comprises of design and synthesis of some newer derivatives by incorporating isoxazole nucleus in the pharmacophore and characterizing them physicochemically and by spectral means. In vitro tube dilution method was followed for their antimicrobial screening against Gram positive bacteria: Staphylococcus aureus, Bacillus subtilis, Gram negative bacteria: Escherichia coli, and two fungal strain: Candida albicans and Aspergillus niger respectively. The results indicated that compound TPI-2, TPI-5 and TPI-14 were found to be the most active antibacterial and antifungal agents respectively.