An efficient multi component reaction for the synthesis of new 3-(2-amino-6-arylpyrimidin-4-yl)-4-hydroxyquinolin-2(1H)-ones has been described. Synthesized derivatives were screened for their in vitro antimicrobial and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity. Among the tested compounds 3 k, 3 m and 3 r shown better antibacterial properties and have displayed broad spectrum of activity than Neomycin against Staphylococcus aureus, Bacillus cereus, Klebsiella planticola, Escherechia coli, S.aureus and Pseudomonas aeruginosa. Moreover 3 r, 3 t and 3 n were found to have potent antifungal activity against Candida parapsilosis, Candida albicans, Aspergillus niger, Candida glabrata, Issatchenkia hanoiensis and Candida than the standard Miconazole. Furthermore 3 c, 3 j, 3 d, 3 m, and 3 h showed strong DPPH free radical scavenging activity than Ascorbic acid. © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim