The synthesis of novel chalcone derivatives [C1-C5] using the ClaisenSchmidt condensation method is part of this work. Subsequently, chalcones were treated with guanidine hydrochloride, urea, thiourea, and thioacetamide, respectively, in the presence of ethanolic sodium hydroxide to create new heterocyclic derivatives, including pyrimidines [Ca1-Ca5], 2-amino-1,3-oxazines [Cb1-Cb5], 2-amino-1,3thiazines [Cd1-Cd5], and 2-methyl-1,3-thiazines [Cd6-Cd10]. The target compounds' synthetic chemical structures have been inferred through the use of mass spectral, 1H NMR, 13C NMR, and FT-IR data. The antioxidant and antibacterial properties of each recently created compound have been examined. The novel-produced compounds' antioxidant activity was assessed using the DPPH. Compounds Ca3, Ca4, Ca5, and Cd5 have DPPH radical scavenging properties that are especially potent and equivalent to ascorbic acid. In an antibacterial study, it was found that the synthetic compounds C2, C5, Cb1, Cb2, Cb4, Cd1, Cd2, Cd6, Cd8, and Cd9 were more effective than Gentamycin as a control medicine against Staphylococcus aureus.