In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be a severe problem. Thus with the aim of developing novel molecules with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance, herein we report the synthesis of thiazolyl triazole derivatives, starting from ethyl acetoacetate, by microwave organic reaction enhancement method (MORE) and results of investigations of their antimycobacterial and antimicrobial activities. Many compounds have shown promising activity while others were inactive.