a Department of Chemistry , Faculty of Sciences, Karadeniz Technical University , Trabzon , Turkey.
b Department of Genetic and Bioengineering , Faculty of Engineering and Natural Sciences, Gümüşhane University , Gümüşhane , Turkey , and.
J Enzyme Inhib Med Chem. 2016;31(sup3):89-95. doi: 10.1080/14756366.2016.1206088. Epub 2016 Jul 18.
Compound 2 was synthesized by reacting CS/KOH with compound 1. The treatment of compound 2 with hydrazine hydrate produced compound 3. Then, compound 3 was converted to Schiff bases (4a-d) by the handling with several aromatic aldehydes. The treatment of triazole compounds 4a-d containing Schiff base with morpholine gave compounds 5a-d. All compounds were tested for their antioxidant and antimicrobial activities. The antioxidant test results of DPPH• radical scavenging and ferric reducing/antioxidant power methods showed good antioxidant activity. The triazole-thiol (3) was the most active, and the effect of the substituent type of the thiophene ring on the activity was same for both Schiff bases (4a-d) and Mannich bases (5a-d). Among the newly synthesized triazole derivatives, the Schiff base 4d and the Mannich base 5d carrying nitro substituent on the thiophene ring showed promising antibacterial and antifungal activity, with lower MIC values than the standard antibacterial ampicillin.
化合物 2 通过 CS/KOH 与化合物 1 反应合成。用肼水合物处理化合物 2 得到化合物 3。然后，化合物 3 通过与几种芳香醛处理转化为席夫碱（4a-d）。用吗啉处理含席夫碱的三唑化合物 4a-d 得到化合物 5a-d。所有化合物均进行抗氧化和抗菌活性测试。DPPH•自由基清除和铁还原/抗氧化能力法的抗氧化测试结果表明具有良好的抗氧化活性。三唑-硫醇（3）活性最高，噻吩环取代基类型对席夫碱（4a-d）和曼尼希碱（5a-d）的活性影响相同。在新合成的三唑衍生物中，噻吩环带有硝基取代基的席夫碱 4d 和曼尼希碱 5d 表现出有希望的抗菌和抗真菌活性，其 MIC 值低于标准抗菌氨苄西林。
