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
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
收藏
页码:943 / 955
页数:13
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