A series of furo[3,2-c]pyrones and furo[3,2-c]coumarins agents were efficiently synthesized and structure recognizable proof was performed by FTIR and NMR. The furo[3,2-c]pyrones and furo[3,2-c]coumarins were evaluated against three bacterial strains (Bacillus subtilis, Staphylococcus aureus and Escherichia coli) and two parasitic strains (Aspergillus niger and Candida albicans). The antimicrobial results demonstrated that a couple of compounds showed noteworthy outcomes relating to the standard medications. Compounds 6 b and 9 f indicated great action against Escherichia coli and Bacillus subtilis with MIC value 0.0108 mu mol/ml and 0.0120 mu mol/ml, respectively. Compound 9 f also showed better activity against fungal strains with MIC value 0.0120 mu mol/ml. Based on the outcomes of antimicrobial activities, docking study was performed to know the binding interface of furo[3,2-c]pyrones and furo[3,2-c]coumarins with DNA gyrase topoisomerase II.