Synthesis and evaluation of new phenolic derivatives as antimicrobial and antioxidant agents
作者:Ibrahim Chaaban、El Sayeda M. El Khawass、Heba A. Abd El Razik、Nehad S. El Salamouni、Doaa A. Ghareeb、Abeer E. Abdel Wahab
DOI:10.1007/s00706-017-1983-z
日期:2018.1
AbstractNew phenolic derivatives bearing hydrazine and 1,3,4-oxadiazole moieties were synthesized and evaluated for their in vitro antimicrobial and antioxidant activities. Most of the compounds revealed pronounced activity against Pseudomonas aeruginosa as well as promising antioxidant activities. N 1-(2,5-Dihydroxybenzoyl)-N 2-(4-methylphenylsulfonyl)hydrazine displayed promising activity against
摘要合成了带有肼和1,3,4-恶二唑部分的新酚类衍生物,并对其体外抗菌和抗氧化活性进行了评估。大多数化合物显示出对铜绿假单胞菌的显着活性以及有希望的抗氧化剂活性。N 1-(2,5-二羟基苯甲酰基)-N 2-(4-甲基苯基磺酰基)肼显示出对大肠杆菌和铜绿假单胞菌有希望的活性。N 1-(2,5-二羟基苯甲酰基)-N 2-(2-萘基亚甲基)肼几乎等同于具有清除活性分别为84%和93%的标准抗氧化剂维生素C。体外细胞毒性研究显示,N 1-(2,5-二羟基苯甲酰基)-N 2-(2,3,4-三甲氧基苯基亚甲基)肼,N 1-(2,5-二羟基苯甲酰基)-N 2-(3,4, 5-三甲氧基苯基亚甲基)肼和N 1-(2,5-二羟基苯甲酰基)-N 2-(4-甲基苯基磺酰基)肼比参考5-氟尿嘧啶更安全。在计算机药物中,相关特性提出所有化合物均具有高至中等的药物相似性评分。因此,这些衍生物可能是开发有效的抗微生物剂和抗氧化剂的潜在线索。