One of the most important classes of organic compounds present in nature or synthesized in the laboratory is heterocyclic systems. In the treatment of commonly occurring diseases and biological activities these compounds possess an array. Literature survey revealed that Chalcones and Pyrimidines possess a broad spectrum of biological activities like anti-inflamm atory, anti-malarial, antimicrobial, anti-depressant, anti-histamine, anti-tubercular and anti-cancer. This research is an endeavor in this direction of synthesis and characterization of such compounds based on Elemental analysis, IR, 1H NMR and Mass spectroscopy. The pharmacological and anti-bacterial screening of synthesized compounds has also been included. To access many heterocyclic systems containing Nitrogen and Oxygen, chalcones afford a facile route. Hence an attempt is made to synthesize chalcones by the Claisen – Schmidt condensation from 4-Imidazolyl acetophenone with two substituted aromatic aldehydes. After purification and characterization by physical and spectral methods, the resulting chalcones have been converted successfully into Pyrimidines by treatment with Guanidine hydrochloride. Based on the reported literatureby physical and spectral methods the resultant compounds were identified also screened for antibacterial activity.