Synthesis of 1, 3, 4-oxadiazole containing peptidomimetics is described by a p-TsCl/pyridine- mediated cyclization of the corresponding dipeptidyl thiosemicarbazides, which are readily prepared by coupling N-protected amino acid hydrazides with amino acid-derived isothiocyanato esters. Further, the protocol has also been extended for the synthesis of orthogonally protected 1, 3, 4-oxadiazole tethered mimetics as well. The synthetic route is ...