Synthesis of Some Quinoline Oximes by an Efficient Method and their Biological Screening

Fahad T Saleh, Abdul Ahad, Prashant D. Netankar, A. A. Sheikh, S. U. Asema
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Abstract

Quinoline scaffolds have gained substantial interest in the modern era of medicinal chemistry due to their wide range of biological applications. The present work reported the synthesis of various oxime derivatives of quinolines by the reaction of substituted 2-chloro-3-formyl-quinolines with hydroxyl amine hydrochloride. The reaction was mediated by aqueous ethanol, whereas hexamine was used as an efficient, non-toxic and easily available basic organocatalyst. The developed protocol has various advantages, including operational ease, affordability, an eco-friendly approach, and short reaction time. Moreover, the synthesized compounds were subjected to in-vitro antimicrobial activities. The antimicrobial evaluation of almost all the compounds found to be potent and effective. Compounds 4c, 4d, and 4f showed a broad spectrum of inhibition and were more effective when tested against specific Gram (-) and Gram (+) bacteria. In in-vitro antifungal evaluation, all synthesized compounds (4a-4g) showed good sensitivity against the tested fungal cultures except Aspergillus niger
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用高效方法合成一些喹啉肟并对其进行生物学筛选
喹啉支架因其广泛的生物应用而在现代药物化学中获得了极大的关注。本研究通过取代的 2-氯-3-甲酰基喹啉与羟胺盐酸盐反应,合成了各种喹啉肟衍生物。反应由乙醇水溶液介导,而己胺则被用作一种高效、无毒且易于获得的碱性有机催化剂。所开发的方案具有各种优点,包括操作简便、价格低廉、环保和反应时间短。此外,还对合成的化合物进行了体外抗菌活性测试。几乎所有化合物的抗菌效果都很好。化合物 4c、4d 和 4f 的抑菌谱很广,对特定的革兰氏(-)和革兰氏(+)细菌更有效。在体外抗真菌评价中,所有合成化合物(4a-4g)对所测试的真菌培养物均表现出良好的敏感性,黑曲霉除外。
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