مشخصات پژوهش

عنوان	New tacrin e-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-p henyl-4 H -pyrano[2,3- b ]quinoline -3-carboxylates
نوع پژوهش	مقاله چاپ شده
کلیدواژه‌ها	Acetylcholinesterase, Butyrylcholinesterase, Alzheimer's disease, Tacrine
چکیده	A series of poly-functionalized tacrine-derived compounds namely 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates were designed and synthesized as cholinesterases inhibitors. The in vitro inhibition assay against AChE and BuChE demonstrated that most of compounds had potent AChE inhibitory with reserving potential of BuChE inhibition. Among them, compound 6i bearing a 4-(3-bromophenyl) moiety showed the most potent activity against AChE/BuChE (IC50s values of 0.069 and 1.35 μM, respectively). The anti-AChE activity of 6i was five times more than that of tacrine. The SAR study revealed that chloro/bromo substituent at ortho or meta position of the 4-phenyl ring can improve the anticholinesterase activity.
پژوهشگران	علیرضا فرومدی (نفر ششم به بعد)، امید سبزواری (نفر ششم به بعد)، علی اسدی پور (نفر ششم به بعد)، لقمان فیروزپور (نفر ششم به بعد)، سعید امامی (نفر ششم به بعد)، فرشید همایونی مقدم (نفر ششم به بعد)، علیرضا مرادی (نفر پنجم)، محمد مهدوی (نفر چهارم)، حمید ندری (نفر سوم)، یعقوب صرافی (نفر دوم)، محمد اقتداری (نفر اول)