A series of novel compounds N-(4-(2,6-dichloroquinolin-3-yl)-6-(aryl)pyrimidin-2-yl)-2-morpholinoacetamides (5a–l) were synthesized by a series of multistep reactions. Newly synthesized compounds have been characterized by IR, 1 H NMR, 13C NMR, and mass spectral data. Antimicrobial screening of title compounds 5a–l was examined against Gram-positive bacteria (Staphylococcus aureus and Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and three fungi (Candida albicans, Aspergillus niger, and Aspergillus clavatus) by serial broth dilution method. Synthesized compounds showed potent inhibitory action against test organisms. Screened compounds 5e–g and 5i–l were associated with considerably higher antibacterial and antifungal activities than commercially used antibiotics.