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Updated: Jul 15, 2025

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
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芳胺的部分合成:它们的抗尿酶潜力和对接研究

Patricia Akpomedaye Onocha1, Ejike Onwudiegwu Okpala2, Muhammad Shaiq Ali3

  • 1Natural Products/Medicinal Chemistry Unit, Department of Chemistry, University of Ibadan, Ibadan, Nigeria.

Journal of biomolecular structure & dynamics
|October 3, 2023
PubMed
概括

来自Celtis zenkeri的芳香胺衍生物显示出强大的抗尿素酶活性. 乙化产品 (1e) 显示出显著的抑制,这表明对抗尿酸酶的药物发现具有治疗潜力.

关键词:
塞尔蒂斯·赞克里 (Celtis zenkeri) 是一种植物.这是一种N-p-trans-coumaroyltyramine.它具有抗尿素酶活性.芳胺衍生物的芳胺衍生物分子对接的分子对接.

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In the presence of an aqueous base and a halogen, primary amides can lose the carbonyl (as carbon dioxide) and undergo rearrangement to form primary amines. This reaction, called the Hofmann rearrangement, can produce primary amines (aryl and alkyl) in high yields without contamination by secondary and tertiary amines.
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Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
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Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
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