Novel Indole-Isoxazole Hybrids: Synthesis and In Vitro Anti-Cholinesterase Activity

被引：14

作者：

Vafadarnejad, Fahimeh ^{[1
]}

Saeedi, Mina ^{[2
,3
]}

Mahdavi, Mohammad ^{[4
]}

Rafinejad, Ali ^{[1
]}

Karimpour-Razkenari, Elahe ^{[3
]}

Sameem, Bilqees ^{[5
]}

Khanavi, Mahnaz ^{[6
]}

Akbarzadeh, Tahmineh ^{[1
,3
]}

机构：

[1] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, POB 14155-6451, Tehran, Iran

[2] Univ Tehran Med Sci, Fac Pharm, Med Plants Res Ctr, Tehran, Iran

[3] Univ Tehran Med Sci, Persian Med & Pharm Res Ctr, Tehran, Iran

[4] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Res Inst, Tehran, Iran

[5] TUMS IC, Sch Pharm, Int Campus, Tehran, Iran

[6] Univ Tehran Med Sci, Fac Pharm, Dept Pharmacognosy, Tehran, Iran

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2017年 / 14卷 / 06期

关键词：

Acetylcholinesterase; Alzheimer's disease; Butyrylcholinesterase; Heterocycles; Indole; Isoxazole; ACETYLCHOLINESTERASE INHIBITORS; BIOLOGICAL EVALUATION; DOCKING; DESIGN;

D O I：

10.2174/1570180813666161018124726

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: This work reports synthesis and in vitro cholinesterase inhibitory activity of novel indole-isoxazole hybrids. Method: The synthetic procedure was started from different ethyl 5-arylisoxazole-3-carboxylate derivatives. Hydrolysis and reaction of the later compound with tryptamine afforded the desired products in good yields. Conclusion: Among the synthesized compounds, N-(2-(1H-indol-3-yl) ethyl)-5-(2-chlorophenyl) isoxazole-3-carboxamide (4b) showed the best anti-cholinesterase activity.

引用

页码：712 / 717

页数：6

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