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

被引：10

作者：

Acosta, Paola ^{[1
]}

Insuasty, Braulio ^{[1
]}

Abonia, Rodrigo ^{[1
]}

Gutierrez, Margarita ^{[2
]}

Quiroga, Jairo ^{[1
]}

机构：

[1] Univ Valle, Dept Chem, Heterocycl Cpds Res Grp, Cali 25360, Colombia

[2] Univ Talca, Inst Chem Nat Resources, Organ Synth Lab & Biol Act LSO Act Bio, Casilla 747, Talca, Chile

来源：

MOLECULAR DIVERSITY | 2017年 / 21卷 / 04期

关键词：

Pyrazolopyridines; Pyrimidines; Spiropyrimidines; Aromatic aldehydes; Cyclic ketones; Cyclocondensation reaction; 3-COMPONENT SYNTHESIS; ACETYLCHOLINESTERASE INHIBITORS; ARYLIDENE DERIVATIVES; ANTIFUNGAL AGENTS; DESIGN; MALONODINITRILE; ANTIBACTERIAL; MICROWAVE; POTENT;

D O I：

10.1007/s11030-017-9774-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

An efficient route for the synthesis of novel 7-aryl and 7-spiropyrazolo[4', 3':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 IC50 =115-470 mu M

引用

页码：943 / 955

页数：13

共 35 条

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