A series of some novel 2,4-dimethoxy-6-(piperazin-1-yl)-1,3,5-triazine aryl ureido/aryl amido derivatives of biological interest were prepared and screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity. Among all the series of compounds screened, the compounds 5c, 5f, 6c, and 6f were found to have promising anti-inflammatory activity (up to 65–73% TNF-α and 73–85% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (75% TNF-α and 84% IL-6 inhibitory activities at 1μM) while the compounds 5a, 5d, 5e, 6a and 6e found to be potent antimicrobial agent showing even 2 to 2.5- fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 μg/mL.