کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1358802 981363 2014 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Cholinesterase inhibitory activity versus aromatic core multiplicity: A facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines
ترجمه فارسی عنوان
فعالیت مهار کننده کولین استراز در برابر چندگانگی هسته ای معطر: یک سنتز فوری سبز و مطالعات تکاملی مولکولی رپیریدون جدید حاوی تیازولوپیریمیدین
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

Novel thiazolopyrimidine derivatives have been synthesized via microwave assisted, domino cascade methodology in ionic liquid and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Among the newly synthesized compounds 6d, 6a, 6e and 6b displayed higher AChE inhibitory activity than standard drug, galanthamine, with IC50 values of 0.53, 1.47, 1.62 and 2.05 μM, respectively. Interestingly, all the compounds except for 6m–r and 6x displayed higher BChE inhibitory potentials than galanthamine with IC50 values ranging from 1.09 to 18.56 μM. Molecular docking simulations for 6d possessing the most potent AChE and BChE inhibitory activities, disclosed its binding interactions at the active site gorge of AChE and BChE enzymes.

Novel piperidone grafted heterocycles comprising three aromatic core synthesized and evaluated for cholinesterases inhibitory activity to disclose the relationship between the activity and aromatic content of inhibitors.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 2, 15 January 2014, Pages 906–916
نویسندگان
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