当前位置: X-MOL 学术Arab. J. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Benzohydrazide as a good precursor for the synthesis of novel bioactive and anti-oxidant 2-phenyl-1,3,4-oxadiazol-aminoacid derivatives: Structural determination, biological and anti-oxidant activity
Arabian Journal of Chemistry ( IF 6 ) Pub Date : 2024-03-30 , DOI: 10.1016/j.arabjc.2024.105767
Khaled Briki , Talal Lahreche , Mouna Souad Abbassi , Mokhtar Boualem Lahrech , Adil Ali Othman , Ahmed M. Elissawy , Abdel Nasser B. Singab

The synthesis and biological assessment of 2,5-disubstituted-1,3,4-oxadiazole derivatives from benzo hydrazide and amino acids as novel potential antioxidant and antibacterial agents have been reported. The structures of the new compounds were characterized by physicochemical properties and spectral methods. The synthesized compounds were screened for their in vitro antibacterial activity against three Gram-positive bacterial strains, namely ATCC 25923, 14579, ATCC 33090, and two Gram-negative bacterial strains, namely ATCC 27853, ATCC 25922, and antifungal activity against ATCC 10231 in comparison with Amoxicillin, Tetracycline, Gentamicin and Oxacillin as standards. Most of the compounds have excellent efficacy, and some of them, such as , , , , and can inhibit their activity better or very close to that of Amoxicillin, Tetracycline, Gentamicin, Oxacillin used as standards. Compounds and provided good results against with inhibition values of IZ = 14 mm and IZ = 22 mm, respectively, while the rest of the compounds and antibiotics were unable to inhibit it. Compounds , , and showed excellent activity against with values between 31 mm and 34 mm. These results were better than all the standards used. The MIC value (25 µg/ml) for derivatives , and against represent the best activity of the tested compounds. All the target compounds were also screened for radical scavenging antioxidant activities by DPPH, FRAP, and TAC assays and found to be excellent antioxidant agents. According to the results, it was observed that most derivatives synthesized showed excellent activity with a concentration of 250 µg/ml as an antioxidant agent (76 % < RSA < 95.5 %) which gave an inhibition percentage that was better or very close to that of ascorbic acid and better than BHT.

中文翻译:

苯甲酰肼作为合成新型生物活性和抗氧化 2-苯基-1,3,4-恶二唑-氨基酸衍生物的良好前体:结构测定、生物和抗氧化活性

由苯并酰肼和氨基酸合成的 2,5-二取代-1,3,4-恶二唑衍生物作为新型潜在抗氧化剂和抗菌剂的合成和生物学评价已有报道。通过理化性质和光谱方法对新化合物的结构进行了表征。筛选了合成的化合物对三种革兰氏阳性菌株(即 ATCC 25923、14579、ATCC 33090)和两种革兰氏阴性菌株(即 ATCC 27853、ATCC 25922)的体外抗菌活性以及对 ATCC 10231 的抗真菌活性。与阿莫西林、四环素、庆大霉素和苯唑西林作为标准品进行比较。大多数化合物具有优异的功效,其中一些化合物如、、、、、可以更好地或非常接近标准使用的阿莫西林、四环素、庆大霉素、苯唑西林。化合物和抗生素提供了良好的抑制效果,抑制值分别为IZ = 14 mm和IZ = 22 mm,而其余化合物和抗生素不能抑制它。化合物 、 、 和 对 31 mm 和 34 mm 之间的值表现出优异的活性。这些结果优于所有使用的标准。衍生物 和 的 MIC 值 (25 µg/ml) 代表受测化合物的最佳活性。所有目标化合物还通过 DPPH、FRAP 和 TAC 测定筛选了自由基清除抗氧化活性,发现它们是优异的抗氧化剂。根据结果​​,观察到大多数合成的衍生物在浓度为 250 µg/ml 时显示出优异的抗氧化剂活性(76% < RSA < 95.5%),其抑制百分比更好或非常接近抗坏血酸且优于BHT。
更新日期:2024-03-30
down
wechat
bug