A new series of quinoline based aurones 7(a–n) has been synthesized and evaluated for their antibacterial, antifungal and antiquorum sensing activities. These novel aurones have been prepared directly from 2‐chloro‐1‐(2,4‐dihydroxyphenyl)ethan‐1‐one in one pot, by reacting it with differently substituted 2‐chloroquinoline‐3‐carbaldehydes using activated barium hydroxide under solvent free grinding conditions. Structures of these novel aurones are in agreement with their IR, 1H‐NMR, 13C‐NMR and HRMS data. Some of these compounds have attributed a significant antiquorum sensing activity.
Over the past few decades, the dynamic progress in the synthesis and screening of heterocyclic compounds against various targets has made a significant contribution in the field of medicinal chemistry. Among the wide array of heterocyclic compounds, triazole moiety has attracted the attention of researchers owing to its vast therapeutic potential and easy preparation via copper and ruthenium-catalyzed azide-alkyne cycloaddition reactions. Triazole skeletons are found as major structural components in a different class of drugs possessing diverse pharmacological profiles including anti-cancer, anti-bacterial, anti-fungal, anti-viral, anti-oxidant, anti-inflammatory, anti-diabetic, anti-tubercular, and anti-depressant among B. subtilis(MIC) 26a 1.56 µg/mL 26b 3.125 µg/mL 26c 3.125 µg/mL S. aureus(MIC) 26a 1.56 µg/mL 26b 3.125 µg/mL 26c 1.56 µg/mL A. nigar(MIC) 26d 3.125 µg/mL 26e 3.125 µg/mL C. albians(MIC) 26d 3.125 µg/mL 26e 3.125 µg/mL gram negative bacteria(MIC) 26a 3.125 µg/mL 26b 3.125 µg/mL 26c 3.125 µg/mL
The exploration of hybrid molecules for targeting various diseases represents a highly promising approach which has showcased significant momentum worldwide, in the last two decades. Diversely substituted quinoline scaffolds present in naturally occurring bioactive compounds, signify their role in various biological processes and stimulated the research developments around it, for diverse therapeutic applications. With the ongoing search for suitable pharmacophores, the quinoline derivatives have emerged as versatile compounds possessing significant and broad spectrum of biological activities. Further, conjugation of quinoline with other bioactive heterocycles containing oxygen yielded hybrid organic frameworks with improved therapeutic profile leading to an emerging paradigm and tremendous growth in the contemporary drug discovery regime. The synthesis of these hybrid skeletons with high efficiency still remains the most strenuous task and a lot of research work is being performed in this direction. In the present article, we have reviewed the synthetic protocols leading to quinoline‐oxygen heterocycle hybrids and also highlighted the systematic and biological assessment of developed pharmacophores.
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