查尔酮及其衍生物抗菌抗炎活性的合成、表征及生物学评价

Geeta N. Lodhi, A. Nayak
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摘要

化学或药物化学是化学和药理学交汇处的一门学科,涉及药物的设计、方法和制造。查尔酮是一个传统的术语,用于强化含有(E)- 1,3-二苯基丙烷-2-烯-1- 1的化合物,它可以在丙烷链中通过烯烃、酮和羟基的存在而官能化。查尔酮是一类重要的常规化合物,被认为是黄酮类化合物和异黄酮类化合物的前身。合成为(E)-1,3-二苯基丙烷-2-烯-1 -1,其中两个芳香环由一个具有羰基部分和α, β不饱和的三碳键连接。以查尔酮为骨架的化合物具有抗菌、抗炎、镇痛、抗血小板、抗溃疡、抗疟疾、抗癌、抗病毒、抗利什曼原虫、抗氧化、抗结核、抗高血糖、免疫调节、抑制化学介质释放、抑制白三烯B4、抑制酪氨酸酶和醛糖还原酶活性等药理作用。本文主要研究了Claisen Schmidt缩合法合成查尔酮,该缩合法是在稀碱或稀酸的催化下,芳香族醛或酮与脂肪族酮或醛缩合生成α - β -不饱和化合物。本文综述了查尔酮及其衍生物的不同生物学意义,以及它们对细小芽孢杆菌、枯草芽孢杆菌(革兰氏阳性)和大肠杆菌、寻常变形杆菌(革兰氏阴性)的抑菌作用。利用卡拉胶驱动的啮齿动物爪水肿策略评估了16种查尔酮的抗炎作用。
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Synthesis, Characterization and Biological Evaluation of Chalcones and Its Derivatives for Antibacterial and Anti Inflammatory Activity
Chemistry or Medicinal chemistry is a discipline at the Interchange ofchemistry and pharmacology engaged with designing, methodize andcreating drug chalcones is a conventional term given tointensifies bearing the (E)- 1,3-diphenylprop-2-en-1-one, which can befunctionlized in the propane chain by the presence of olefinic, keto as well ashydroxyl group.Chalcones are a significant class of regular items and are considered as the forerunners of flavonoids and isoflavonoids. Synthetically, is (E)-1,3-diphenylprop-2-en-1-one in which two aromatic ring rings are joined by a three carbon bond having a carbonyl moiety and and α, β unsaturation. The compounds with the backbone of chalcones have been accounted for to have different pharmacological activities for example, antimicrobial, anti- inflammatory, analgesic, anti-platelet, anti-ulcerative, antimalarial, anticancer, antiviral, anti-leishmanial, antioxidant, antitubercular, anti-hyperglycemic, immunomodulatory, inhibition of chemical mediators release, inhibition of leukotriene B4, inhibition of tyrosinase and inhibition of aldose reductase activities.  This  paper  mainly  focuses  on  chalcones  synthesized  by Claisen Schmidt condensation which involves the condensation between an aromatic aldehyde or ketone with an aliphatic ketone or aldehyde catalysed by the presence of dilute alkali or acid to form alpha beta unsaturated compound. through reviewing different biological significance of chalcones andtheir derivatives have been reported along with their antibacterial movement against, Bacillus pumilis, Bacillus subtilis (gram-positive) and Escherichia coli, Proteus vulgaris (gram-negative). The antiinflammatory action of the sixteen chalcones has been assessed byutilizing carrageenan-actuated rodent paw oedema strategy.
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