Antimicrobial and cytotoxicity potential of acetamido, amino and nitrochalcones.

Arzneimittel-Forschung-Drug Research Pub Date : 2012-12-01 Epub Date: 2012-10-19 DOI:10.1055/s-0032-1327610
T C Tristão, F Campos-Buzzi, R Corrêa, R C B Cruz, V Cechinel Filho, A Bella Cruz
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引用次数: 7

Abstract

Chalcones constitute one of the major classes of natural products belonging to the flavonoid family, and they have been reported as having a range of important therapeutic activities, including some chalcones are effective as antimicrobial agents. Currently, the search for new structures with antimicrobial activity has been intensified due to the emergence of many strains resistant to antibiotics currently used to treat infectious diseases.3 chalcone series (amino, acetamido and nitrochalcones) were prepared (23 compounds) and evaluated for their antimicrobial and cytotoxic potential. The effects of substituents on their respective activities also was evaluated.The results showed that 4 aminochalcones (2, 4, 8, 9), 3 acetoamidochalcones (10, 14, 18) and 3 nitrochalcones (20, 22, 23), exhibited antifungal effects. The aminochalcones were more toxic than the acetamidochalcones, while the nitrochalcones did not present any toxic effect. It was verified that there seems to be structure-activity correlation in some electron-donating and withdrawing substituents groups in rings A and B of the synthetized chalcone analogues and its antifungal and cytotoxic activity.

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对乙酰氨基、氨基和硝基查尔酮的抗菌和细胞毒性潜力。
查尔酮是类黄酮家族的主要天然产物之一,它们具有一系列重要的治疗活性,包括一些查尔酮是有效的抗菌药物。目前,由于出现了许多对目前用于治疗传染病的抗生素具有耐药性的菌株,对具有抗菌活性的新结构的研究已经加强。制备了3个查尔酮系列(氨基查尔酮、乙酰氨基查尔酮和硝基查尔酮)(23个化合物),并对它们的抗菌和细胞毒性进行了评价。并对取代基对其活性的影响进行了评价。结果表明,4种氨基查尔酮(2,4,8,9)、3种乙酰氨基查尔酮(10,14,18)和3种硝基查尔酮(20,22,23)具有抑菌作用。氨基查尔酮的毒性大于乙酰氨基查尔酮,而硝基查尔酮的毒性不明显。证实了所合成的查尔酮类似物的A环和B环上的一些供电子取代基和吸电子取代基的构效关系及其抗真菌和细胞毒活性。
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