Quinoline derivatives are a group of compounds known to possess a wide range of biological activities. A series of new 2-aryl-quinoline-4-carboxylic acid derivatives were synthesized starting from aniline, different aromatic aldehydes, and pyruvic acid followed by the Doebner reaction. The purity and identities of the synthesized compounds were elucidated through spectroscopic techniques. All of the newly synthesized compounds were characterized by IR and 1H-NMR. The spectral data were interpreted and correlated with the target structures. The synthesized compounds were tested for their antibacterial activity against two Gram +ve strains (Staphylococcus aureus, Bacillus subtilis) and two Gram – ve strains (Klebsiella pneumoniae, Escherichia coli) by Kirby - Bauer Disc Diffusion Method (Zone of inhibition). Among the compounds tested for antimicrobial activity, Furan-2-yl, 2-hydroxyphenyl and 3-methoxy-4-hydroxy phenyl substituted at C2 showed significant activity against Gram +ve and Gram – ve bacteria. Compounds substituted with pyridin-2-yl and 4-nitrophenyl at C2 displayed remarkable activity against both Gram +ve and Gram – ve bacteria.