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In the present study, a series of 5'-(substituted aryl)-2-furanyl}-3,4-dihydro-7/-/-pyrimidine-2-ones has been designed and synthesized with Beginelli reaction derivatives carried out from the reaction of ethyl acetoacetate 1 with substituted ureas 2 and substituted aryl furfuraldehydes 3 in presence of acetic acid to yield {5'-(substituted aryl)- 2-furanyl}-3,4-dihydro-7H-pyrimidine-2-ones [4a-k (X=O), 4l-v (X=S)]. The target candidates were confirmed by FTIR, NMR, Mass spectrometry and by elemental analysis. The present exploration also required for in vitro antibacterial activity against Gram-positive strains of bacteria, namely Bacillus cereus (ATCC 11778), Staphylococcus aureus (ATCC 11633), Staphylococcus epidermidis (ATCC 155), Enterococccus faecalis (ATCC 14506) and Gram negative bacterial strains, namely Shigella dysenteriae (ATCC 13313), Escherichia coli (ATCC11303), Klebsiella pneumoniae (ATCC 10031) and Salmonella typhi (MTCC 733). Tested antimicrobial activity revealed that compounds 4k and 4v showed very promising antibacterial activity and were found to be most effective when tested against strains of K. pneumonia, S. aureus, S. typhi, S. epidermidis and E. faecalis, although rest synthesized derivatives also showed significant antibacterial activity. The novel synthesized compounds also exerted remarkable in vitro anti-inflammatory biological activity as reflected by utilization of the percent inhibition of protein denaturation method. [ABSTRACT FROM AUTHOR]