In this research article we synthesized 1,2,4 (H) triazole 3-amine as a core molecule from aminoguinidine and formic acid in basic medium sodium 0 carbonate heated at 120-123 C for 12 h. It has excellent medicinal application. In synthetic modication especial emphasis on free –NH as a20 pharmacophore which is synthetically active group. A series of 03 innovative molecules were synthesized by isocyanate in ethanol solvent at 0 C to room temperature, 2 h. Urea as important moiety found in synthesized molecule. The purity of all compounds will be checked by TLC and wherever found necessary the compounds will be puried by column chromatography. The structure of all compounds will be established on the 1 13 basis of microanalysis, FTIR, HNMR, CNMR, DEPT and mass spectral data. Antibacterial and antifungal evaluation of synthesized derivatives in vitro has done by Kirby Bauer Method. NCIM provides pure, non-pathogenic, viable and authentic cultures with their standard code number and testing symbols; Ciprooxacin (10 lg) and uconazole (5 lg) were used as standard antibacterial and antifungal drugs, respectively. Minimum zone of inhibition & % activity has been determined; from these values its predicted that antibacterial value of the derivatives are more prominent that core molecule against Gram positive bacterial strains Staphylococcus aureus & Bacillus subtilis. Antifungal activity is more prominent in TZA2 derivative where urease moiety connected with cyclohexyl group against Aspergillus niger & Penicillium Chrysogenum