Temüz Mehmet Mürşit, Çankaya Nevin, Korcan Safiye Elif, Yalçin Azarkan Serap, Kahraman Tuğba
Department of Chemistry, Firat University, Faculty of Science, Elazığ 23119, Turkey.
Vocational School of Health Services, Usak University, Usak 64200, Turkey.
ACS Omega. 2024 Feb 9;9(7):7910-7922. doi: 10.1021/acsomega.3c07836. eCollection 2024 Feb 20.
The antibacterial, antifungal, and antioxidant activities of 2-chloro--(4-methoxyphenyl)acetamide (-acetamide) and 2-(4-methoxyphenylamino)-2-oxoethyl methacrylate (MPAEMA) were investigated by experiments and analyses. MPAEMA has an antibacterial effect only against Gram-positive . It was determined that this did not affect any other bacteria and yeast. On the other hand, -acetamide showed antimicrobial activity against ATCC 25923, ATCC 90030, NRRL 744, ATCC 551289, ATCC 25922, NRLLB4420, ATCC 27853, and ATCC 1911. -Acetamide showed the greatest antifungal effect by inhibiting the colony growth of (98%). This was followed by with 83% and with 21%. MPAEMA inhibited colony growth of by 95% and that of by 91%. Also, -acetamide and MPAEMA had a scavenging effect on free radicals. According to results of the analysis, the antimicrobial effect of these compounds is due to their effect on DNA ligase. Based on drug-likeness analysis, they were found to be consistent with the Lipinski, Veber, or Ghose rule. -Acetamide and MPAEMA may be used as drugs.
通过实验和分析研究了2-氯-（4-甲氧基苯基）乙酰胺（α-乙酰胺）和甲基丙烯酸2-（4-甲氧基苯基氨基）-2-氧代乙酯（MPAEMA）的抗菌、抗真菌和抗氧化活性。MPAEMA仅对革兰氏阳性菌有抗菌作用。已确定其对任何其他细菌和酵母均无影响。另一方面，α-乙酰胺对金黄色葡萄球菌ATCC 25923、大肠杆菌ATCC 90030、酿酒酵母NRRL 744、白色念珠菌ATCC 551289、肺炎克雷伯菌ATCC 25922、近平滑念珠菌NRLLB4420、粪肠球菌ATCC 27853和黑曲霉ATCC 1911显示出抗菌活性。α-乙酰胺通过抑制白色念珠菌的菌落生长（98%）显示出最大的抗真菌作用。其次是热带念珠菌，抑制率为83%，光滑念珠菌为21%。MPAEMA对白色念珠菌的菌落生长抑制率为95%，对热带念珠菌的抑制率为91%。此外，α-乙酰胺和MPAEMA对自由基有清除作用。根据分子对接分析结果，这些化合物的抗菌作用归因于它们对DNA连接酶的作用。基于类药性分析，发现它们符合Lipinski、Veber或Ghose规则。α-乙酰胺和MPAEMA可作为药物使用。
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