New derivatives of 8-Chloro-theophylline (8-CTh) were synthesized by react 8-CTh and 4-amino acetophenone to prepared 8-(4-acetylphenylamino)-1,3-dimethyl-1H-purine-2,6(3H,7H)dione then the result reacts with some substituted benzaldehyde derivatives to prepared different chalcone compound then the products were allowed to react with thiourea and hydrazine to give Pyrimidine and pyrazoline derivatives respectively. The reaction was monitored by thin layer chromatography (TLC) technique. All new compounds were characterized by melting points, elemental analysis, FTIR, 1 H, 13 C and 2D NMR spectroscopy. Antimicrobial activity of these derivatives was also determined.