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具有表面活性和生物活性的吡啶及相关杂环体系的合成与杂环化

Synthesis and Heteroannulation of Pyridine and Related Heterocyclic Systems Having Surface and Biological Activities.

作者信息

El-Sayed Refat

机构信息

Chemistry Department, College of Applied Sciences, Umm Al-Qura University.

出版信息

J Oleo Sci. 2015;64(7):761-74. doi: 10.5650/jos.ess15011.

DOI:10.5650/jos.ess15011
PMID:26136175
Abstract

Possible approaches to the synthesis of functionalized, pyrazole, isoxazole, pyrimidine, pyridine and fused pyridine derivatives The sequence involves the heterocyclization of ethyl 3-oxo-2-(4-stearamidobenzoyl)butanoate (3) with appropriate reagents. Propoxylated of these heterocycles using propylene oxide to produce nonionic surface active agents having a long alkyl chain with molecular weight suitable for becoming an amphiphilic molecule with correct hydrophilic-lypophilic balance which enhances solubility, biodegradability and hence lowers the toxicity to human beings and becomes environmentally friendly. The antimicrobial activity of the newly synthesized was examined and it was found that some of these compounds have similar or higher activity compared with commercial antibiotic drugs (sulphadiazine), which make them suitable for diverse applications like the manufacturing of drugs, pesticides, emulsifiers, cosmetics, etc.

摘要

合成功能化吡唑、异恶唑、嘧啶、吡啶及稠合吡啶衍生物的可能方法 该序列涉及3-氧代-2-(4-硬脂酰胺基苯甲酰基)丁酸乙酯(3)与适当试剂的杂环化反应。使用环氧丙烷对这些杂环进行丙氧基化,以生产具有长烷基链的非离子表面活性剂,其分子量适合成为具有正确亲水亲油平衡的两亲分子,从而提高溶解性、生物降解性,进而降低对人类的毒性并变得环境友好。对新合成的化合物的抗菌活性进行了检测,发现其中一些化合物与市售抗生素药物(磺胺嘧啶)相比具有相似或更高的活性,这使得它们适用于多种应用,如药物制造、农药、乳化剂、化妆品等。

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