Utilisation of bis-chloroacetamide derivative in the synthesis of new biologically active sulfide compounds

IF 0.8 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY South African Journal of Chemistry-Suid-Afrikaanse Tydskrif Vir Chemie Pub Date : 2022-01-01 DOI:10.17159/0379-4350/2021/v76a14
Ehab Norhan A Khalaf, Abdel-Latif, M. Ismail, H. Metwally, E. Abdel‐Latif
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Abstract

4-Aminobenzohydrazide (1) undergoes chloroacetylation twice, at the primary amine and hydrazide-NH2 functional groups. The conforming bis-chloroacetamide derivative 3 was reacted with different sulfur reagents (namely, 2-mercaptobenzothiazole, 6-amino-2-mercaptopyrimidin-4-ol, and 2-mercapto-4,6-dimethyl-nicotinonitrile) to give new bis-sulfide compounds 5, 7 and 9, respectively. The newly synthesised bis-chloroacetamide and corresponding sulfides were screened for anti-microbial and antioxidant potential. The sulfide derivative 7 exhibited the most potent activity against Staphylococcus aureus and Pseudomonas aeruginosa. It shows inhibition activities of 83.4% and 78.8%, respectively. Moreover, the sulfide derivative 7 showed the highest antioxidant activity with an inhibition ratio of 85.9%, which is close to L-ascorbic acid.
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利用双氯乙酰胺衍生物合成新的生物活性硫化物
4-氨基苯并肼(1)在伯胺和肼- nh2官能团上经历了两次氯乙酰化。符合条件的双氯乙酰胺衍生物3与不同的含硫试剂(即2-巯基苯并噻唑、6-氨基-2-巯基嘧啶-4-醇和2-巯基-4,6-二甲基-烟腈)反应,分别得到新的双硫化物5、7和9。对新合成的双氯乙酰胺及其相应的硫化物进行了抗菌和抗氧化活性筛选。其中硫化物衍生物7对金黄色葡萄球菌和铜绿假单胞菌的活性最强。其抑制活性分别为83.4%和78.8%。硫化物衍生物7的抗氧化活性最高,抑制率为85.9%,与l -抗坏血酸相近。
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来源期刊
CiteScore
3.10
自引率
0.00%
发文量
6
审稿时长
>12 weeks
期刊介绍: Original work in all branches of chemistry is published in the South African Journal of Chemistry. Contributions in English may take the form of papers, short communications, or critical reviews.
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