TY - JOUR AU - Ezugwu, James A. AU - Ezeokonkwo, Mercy A. AU - Okafor, Sunday N. AU - Godwin-Nwakwasi, Evelyn U. AU - Ibeanu, F. N. PY - 2017/12/22 Y2 - 2024/03/29 TI - Palladium-Catalyzed Sonogashira Synthesis of Alkynyl Derivatives of Quinoline-5, 8-Dione JF - Asian Journal of Applied Sciences JA - AJAS VL - 5 IS - 6 SE - Articles DO - UR - https://www.ajouronline.com/index.php/AJAS/article/view/4987 SP - AB - <p>The synthesis of various alkynylquinoline-5,8-diones is reported. The intermediate 6,7-dibromoquinoline-5,8-dione was obtained by nitrosation of 8-hydroxyquinoline, followed by reduction and subsequent bromination and oxidation. The coupling reaction of 6,7-dibromoquinoline-5,8-dione with various terminal alkynes via Palladium catalysis gave the alkynylquinoline-5,8-diones in good to excellent yields (50-85% ). The chemical structures of the products were confirmed using spectroscopic methods, which include UV/Visible spectrophotometer, Fourier Transform-Infrared (FT-IR) Spectroscopy, <sup>1</sup>H and <sup>13</sup>C-NMR Spectroscopy. In vitro antimicrobial activity screening carried out on the compounds against bacterial strains: Escherichia coli 1, Escherichia coli 12, Staphylococcus aureus, Klebsiella pneumonia and Pseudomonas aeroginosa, showed that the synthesized compounds have significant activities (MIC= 0.15-3.20), against the tested organisms. However, compound 5e did not inhibit the growth of Pseudomonas aeroginosa.<em> </em></p> ER -