A number of (1H-1, 2, 3-triazol-1-yl) benzo [d] thiazoles were synthesized utilizing a versatile Cu-catalyzed azide–alkyne click reaction (CuAAC) on tautomeric benzo [4, 5] thiazolo [3, 2- d] tetrazole (1) and 2-azidobenzo [d] thiazole (2) starting materials. Moreover, one of the resulting products of this investigation, triazolbenzo [d] thiazole 22, was found to possess significant neuroprotective activity in human neuroblastoma (SH-SY5Y) cells.