We have synthesized protected mannofuranose as a glycosyl donor and some heterocyclic moieties as glycosyl acceptor. Coupling of glycosyl donor and acceptor by glycosylation, results in the formation of mannofuranoside derivatives. Antimicrobial potential of synthesized compounds were tested against five different human pathogenic bacteria and two fungi by using microdilution method. Interestingly, all synthesized mannofuranoside derivatives gave antimicrobial activity. Cumulatively, inhibitory concentration (IC 50 ) against bacteria were found to be in the range of 84.28-309.43 μg/ml, while, IC 50 against fungus were in the range of 0.59-3.82 mg/ml. Ampicillin and Fluconazole were used as positive control. Further, physicochemical parameters of synthesized mannofuranoside derivatives were analyzed using in-silico approach. Fortunately, none of our synthesized mannofuranoside derivatives gave violation of Lipinski's Rule of Five. Thus, we can safely state that these synthesized mannofuranoside derivatives could be considered as potential anti-microbial drug candidates.