The use of chemicals (drugs) for both medical and recreational purposes is hardly new. In fact, drug use seems to have been a part of human science prehistory. Morpholine (C4H9NO, 1-oxa-4- azacyclohexane) is a synthetic simple heterocyclic organic compound having characteristic functional groups of amine and ether and great industrial importance. Chemical manipulations on morpholine based molecules through structure - activity relationship strategy could help developing many interesting candidates of therapeutic significance to tackle broad range of medical ailments. Feasible physicochemical properties (polarity and solubility), low cost and wide availability make it a suitable candidate for the synthesis of many potent drugs.