In the design of new bioactive compounds, the development of hybrid molecules through the combination of different pharmacophores in one frame may lead to compounds with interesting biological profiles. Serial of the “1-aryl-5-para-tolyl 2-s-benzyl-2-4-isodithiobiurets”was prepared by the interaction of 1-aryl-s-benzyl-isothiocarbamide and P-tolyl-isothiocynate in Benzene Medium. The Reaction was refluxed for 3-hours in benzene medium. After completion of the reaction, the solvent was distilled off and sticky residue obtained was triturated with petroleum ether (60-80oC) to afford a pale yellow solid (IIIa). It was purified by chloroform-petroleum ether (IIIa), m.p. 1700C. The elemental analysis of this new product indicated molecular formula as C22H21N3S2 Acylureas and biurets are noncyclic compounds which upon replacement of one or both oxygen with sulphur results into the formation of thiobiurets and dithiobiurets respectively. Isodithiobiuret derivatives shows potent biological activities such as anticonvulsant, hypnotic, analgesic, antifungal, insecticidal activity.