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Synthesis, Antibacterial and Antioxidant Activities of Some New Nsubstituted Azachalcone, Schiff base and Pyrazole Derivatives
Letters in Organic Chemistry ( IF 0.8 ) Pub Date : 2020-07-31 , DOI: 10.2174/1570178617666200108111211
Nedime Çalışkan 1 , Asu Usta 1 , Fatih Şaban Beriş 2 , Nimet Baltaş 1 , Efsun Çelik 2
Affiliation  

Pyrazoles, Schiff bases and the quaternary ammonium compounds (QAC) such as N-alkyl substituted azachalcones are the important group of chemical individuals with widespread usage in many fields of science. In particular, these compounds have proven biological activities. In addition, the emergence of resistance against antibiotics used is the cause of an increasing necessity of new effective substances. Therefore, new N-alkyl substituted derivatives (4-7), 1,3,5-trisubstituted-2- pyrazoles (8-10) and Schiff bases (11-13) with biological activities such as phenolic. antioxidants or QAC were synthesized, starting from azachalcones. The structures of the compounds were elucidated with spectral methods including IR, 1H-NMR, 13C-NMR, COSY spectral data and elemental analyses. The prepared compounds were evaluated for antibacterial activity against four Gram-positive bacteria, and four Gram-negative bacteria. The minimum inhibitory concentration (MIC) of the N-alkylated azachalcone derivatives 5 and 7 (7.8 mg/mL) showed strong antimicrobial activities, especially against Bacillus cereus. Antioxidant capacities of the synthesized compounds were determined by using CUPRAC and FRAP methods. As a result, compound 9 was observed to be more effective than other compounds.



中文翻译:

某些新的N取代的Azachalcone,Schiff碱和Pyrazole衍生物的合成,抗菌和抗氧化活性

吡唑,席夫碱和季铵化合物(QAC),例如N-烷基取代的氮杂双氮杂环丁烷是重要的化学物种,在许多科学领域中都有广泛的用途。这些化合物尤其具有已证明的生物学活性。另外,对所用抗生素的抗药性的出现是新有效物质需求增加的原因。因此,具有生物活性例如酚醛的新的N-烷基取代的衍生物(4-7),1,3,5-三取代-2-吡唑(8-10)和席夫碱(11-13)。抗氧化剂或QAC是从天青石烯开始合成的。用光谱方法阐明了化合物的结构,包括IR,1 H-NMR,13 C-NMR,COZY光谱数据和元素分析。评价所制备的化合物对四种革兰氏阳性细菌和四种革兰氏阴性细菌的抗菌活性。N-烷基化氮杂硫唑酮衍生物5和7的最低抑菌浓度(MIC)(7.8 mg / mL)显示出很强的抗菌活性,尤其是对蜡状芽孢杆菌。合成的化合物的抗氧化能力通过使用CUPRAC和FRAP方法确定。结果,观察到化合物9比其他化合物更有效。

更新日期:2020-07-31
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