双取代İsovanillin衍生物的抗菌和抗氧化活性评价

Zehra Tekin, Yener Tekeli̇, Zehra Küçükbay, Nebih Lolak, G. Yapar, Suleyman Akocak
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摘要

本文利用双醛类化合物与取代的肼类化合物的反应,重新合成了一系列12个双腙取代异香草碱衍生物3(a- 1),因为这些化合物先前表现出了强效的醛糖还原酶抑制作用。对所得化合物进行了潜在的抗菌和抗氧化活性测试。本研究采用革兰氏阳性菌株(金黄色葡萄球菌ATCC 29213、粪肠球菌ATCC 29212)和革兰氏阴性菌株(铜绿假单胞菌ATCC 10231、大肠杆菌ATCC 25912)。另一方面,采用DPPH自由基清除法、TEAC铜还原法和金属螯合活性法测定了新合成的双腙取代异香草碱衍生物的抗氧化能力。一些铅分子被发现是对金黄色葡萄球菌和大肠杆菌菌株的潜在细菌抑制剂。更具体地说,化合物3g (R=-H)和3j (R= -4Cl)对大肠杆菌菌株具有良好的抑制作用,其MIC值分别为1.56和6.25µg/mL。此外,与比较标准相比,没有一种化合物对测试方法显示出有效的抗氧化活性。
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Antibacterial and Antioxidant Activity Evaluation of Bis-Substituted İsovanillin Derivatives
Herein, a series of twelve bis-hydrazone substituted isovanilline derivatives 3(a-l), were freshly re-synthesized by the reaction of bis-aldehydes with substituted hydrazide derivatives since these compounds previously showed potent aldose reductase inhibition properties. The obtained compounds were tested for their potential antibacterial and antioxidant activities. In the present study, four different bacterial strains were used, including Gram-positive (Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212) and Gram-negative (Pseudomonas aeruginosa ATCC 10231, Escherichia coli ATCC 25912). On the other hand, the antioxidant capacities of freshly re-synthesized bis-hydrazone substituted isovanilline derivatives were determined by using several antioxidant methods, including DPPH free radical scanvenging, TEAC cupric reducing (CUPRAC) and metal chelating activity methods. Several lead molecules were discovered as a potential bacterial inhibitors against S. aureus and E. coli bacterial strains. More specifically, compounds 3g (R=-H) and 3j (R= -4Cl) showed great inhibition properties against E. coli bacterial strains by having MIC values of 1.56 and 6.25 µg/mL, respectively. Moreover, none of the compounds showed potent antioxidant activity against tested methods with respect to compared standards.
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