Benzothiazole are important group of compounds reported to have various biological activities and hence the present study was undertaken in order to synthesize same new compounds built upon this nucleus with the hope to enhance the biological properties of newly designed compounds. In the present work 2-substituted benzothiazole (a) was prepared from p-tolnidine via cyclization reaction then N-2-benzothiazolyl thiourea was synthesized by reacting (a) with ammonium thiocyanate. Then its semicarbazide derivative was formed reacting with hydrazine hydrate in ethylene glycol which was reacted with various acetophenons to form respective derivatives. Chemical structure of product and their purity was ascertained by TLC, MP and various spectral methods as FTIR and NMR. The inhibition of microorganism under standard condition was determined to demonstrate antimicrobial activity of derivatives using gram positive and gram negative bacteria such as Staphylococcus aureus, Pseudomonas. aeruginosa,, Escherichia coli with ampicillin as standard compounds. IR and NMR spectral data were supporting the presence of synthesized compounds. Derivatives showed significant zone of inhibition against the both gram positive and gram negative bacteria. The metanitroacetophenone derivative showed excellent activity against P. aeruginosa.