Medicinal chemist are striving to arrive at a promising anti-tubercular agents which can be effective against XDR & MDR tuberculosis. This has made them to work non-conventionally to arrive at promising “Hit”. This article describes synthesis and antimycobacterial activity of clubbed thiazolyl-triazole molecule which are synthesised overriding the Lipinski rule of five. The compounds have shown potency comparable with isoniazid even with 25 XDR & MDR clinical isolates. The candidate is under further development status and is showing promising activity with minimal toxicity.