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新型 7-芳基和 7-螺吡喃并[4',3':5,6]吡啶并[2,3-d]嘧啶衍生物的合成及其作为乙酰胆碱酯酶抑制剂的研究。

Synthesis of novel 7-aryl and 7-spiropyrazolo[4',3':5,6]pyrido[2,3-d]pyrimidine derivatives and their study as AChE inhibitors.

机构信息

Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A.A. 25360, Cali, Colombia.

Organic Synthesis Laboratory and Biological Activity (LSO-Act-Bio), Institute of Chemistry of Natural Resources, Universidad de Talca, Casilla 747, Talca, Chile.

出版信息

Mol Divers. 2017 Nov;21(4):943-955. doi: 10.1007/s11030-017-9774-3. Epub 2017 Aug 7.

Abstract

An efficient route for the synthesis of novel 7-aryl and 7-spiropyrazolo[4[Formula: see text],3[Formula: see text]:5,6]pyrido[2,3-d]pyrimidine derivatives is described. These compounds were obtained by a cyclocondensation reaction between pyrazolopyridinediamines 4 and aldehydes 5 or cyclic ketones 6 in the presence of acetic acid as catalyst. This procedure provides the desired compounds in good yields under a simple two-step methodology. The obtained compounds were evaluated as AChE inhibitors and showed weak AChe inhibition with [Formula: see text].

摘要

描述了一种新型 7-芳基和 7-螺吡唑并[4,3-e][1,3,4]噻二唑并[2,3-d]嘧啶衍生物的有效合成路线。这些化合物是通过吡唑并吡啶二胺 4 与醛 5 或环状酮 6 在乙酸作为催化剂的存在下进行环缩合反应得到的。该方法在简单的两步法中以良好的收率得到了所需的化合物。所得到的化合物被评价为 AChE 抑制剂,并且与[Formula: see text]显示出弱的 AChE 抑制活性。

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