Carbohydrates are the most abundant and the most diverse biopolymers in nature. Due to the importance of carbohydrates it is necessary to develop a new method for the synthesis of carbohydrate based drugs of the current global situation for health and disease. In this present work we demonstrate the synthesis of methyl 4,6-O-benzylidene-ɑ-D-glucopyranoside derivatives by direct acylation method. The structures of the newly prepared compounds have been characterized and elucidated using various physico-chemical and spectroscopic methods including elemental analysis, melting point determination, infrared and proton NMR spectroscopy. A number of acyl derivatives were prepared in order to obtain a series of newer components for antibacterial screening experiments. These acylated derivatives were evaluated for in vitro antibacterial screening studies against four human pathogenic bacteria by disc diffusion method.