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Pharmacological Evaluation and Docking Studies of 3-Thiadiazolyl- and Thioxo-1,2,4-triazolylcoumarin Derivatives as Cholinesterase Inhibitors
المؤلفون المشاركون
Saeed, Aamer
Iqbal, Jamshed
Muddassar, Muhammad
Khan, Aftab Ahmad
Raza, Ahsan
Ibrar, Aliya
المصدر
العدد
المجلد 2012، العدد 2012 (31 ديسمبر/كانون الأول 2012)، ص ص. 1-11، 11ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2012-08-16
دولة النشر
مصر
عدد الصفحات
11
التخصصات الرئيسية
العلوم الطبية والصيدلة والعلوم الصحية
علم الصيدلة
الملخص EN
Inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is considered a promising strategy for the treatment of Alzheimer’s disease (AD).
This research project aims to provide a comprehensive knowledge of newly synthesized coumarin analogues with anti-AD potential.
In the present work a series of 3-thiadiazolyl- and thioxo-1,2,4-triazolylcoumarins derivatives were designed, synthesized, and tested as potent inhibitors of cholinesterases.
These compounds were assayed against AChE from electrophorus electricus and rabbit; and BChE from horse serum and rabbit by Ellman’s method using neostigmine methylsulphate and donepezil as reference drugs.
Some of the assayed compounds proved to be potent inhibitors of AChE and BChE with Ki values in the micromolar range.
4b was found to be the most active compound with Ki value 0.028±0.002 μM and higher selectivity for AChE/BChE.
The ability of 4b to interact with AChE was further confirmed through computational studies, in which a primary binding was proved to occur at the active gorge site, and a secondary binding was revealed at the peripheral anionic site.
Structure activity relationships of prepared compounds were also discussed.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Raza, Ahsan& Saeed, Aamer& Ibrar, Aliya& Muddassar, Muhammad& Khan, Aftab Ahmad& Iqbal, Jamshed. 2012. Pharmacological Evaluation and Docking Studies of 3-Thiadiazolyl- and Thioxo-1,2,4-triazolylcoumarin Derivatives as Cholinesterase Inhibitors. ISRN Pharmacology،Vol. 2012, no. 2012, pp.1-11.
https://search.emarefa.net/detail/BIM-492208
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Raza, Ahsan…[et al.]. Pharmacological Evaluation and Docking Studies of 3-Thiadiazolyl- and Thioxo-1,2,4-triazolylcoumarin Derivatives as Cholinesterase Inhibitors. ISRN Pharmacology No. 2012 (2012), pp.1-11.
https://search.emarefa.net/detail/BIM-492208
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Raza, Ahsan& Saeed, Aamer& Ibrar, Aliya& Muddassar, Muhammad& Khan, Aftab Ahmad& Iqbal, Jamshed. Pharmacological Evaluation and Docking Studies of 3-Thiadiazolyl- and Thioxo-1,2,4-triazolylcoumarin Derivatives as Cholinesterase Inhibitors. ISRN Pharmacology. 2012. Vol. 2012, no. 2012, pp.1-11.
https://search.emarefa.net/detail/BIM-492208
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-492208
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
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