Application of PEG-400 as a green biodegradable polymeric medium for the catalyst-free synthesis of spiro-dihydropyridines and their use as acetyl and butyrylcholinesterase inhibitors |
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| Affiliation: | 1. Department of Chemistry, Faculty of Sciences, Persian Gulf University, Bushehr 75169, Iran;2. The Persian Gulf Marine Biotechnology Research Center, the Persian Gulf Biomedical Research Center, Bushehr University of Medical Sciences, Bushehr, Iran;3. Department of Plant Production and Breeding Engineering, Faculty of Engineering and Technology, Imam Khomeini International University, Qazvin, Iran;1. Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII 27-31, 08028 Barcelona, Spain;2. Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom;3. Bradford School of Pharmacy, University of Bradford, West Yorkshire BD7 1 DP, United Kingdom;4. Department of Pharmaceutics, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana;5. Departament de Farmacologia, de Terapèutica i de Toxicologia, Universitat Autònoma de Barcelona, 08193-Bellaterra, Barcelona, Spain;1. Kazan (Volga region) Federal University, Kremlyovskaya 18, 420008 Kazan, Russia;2. A.E. Arbuzov Institute of Organic and Physical Chemistry; KazSC, Russian Academy of Sciences, Arbuzova 8, 420088 Kazan, Russia;3. Institute of Physiologically Active Compounds of Russian Academy of Sciences, Severnyi pr. 1, Chernogolovka, Moscow Reg. 142432, Russia;4. Kazan Institute of Biochemistry and Biophysics, Lobachevsky St. 2/31, Kazan 420111, Russia;1. Alchemical Research, LLC, 260 East Wall Street, Bethlehem, PA 18018, USA;2. Division of Pharmaceutical Sciences, School of Pharmacy, and Department of Chemistry, University of Wisconsin, Madison, WI 53705, USA;1. College of Pharmacy, Catholic University of Daegu, Gyeongbuk 712-702, Republic of Korea;2. Korean Bioinformation Center (KOBIC), Daejeon 305-806, Republic of Korea;3. College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 702-701, Republic of Korea;4. Faculty of Food Science and Biotechnology, Pukyung National University, Busan 608-737, Republic of Korea;1. Laboratory of Natural Products and Organic Synthesis, Department of Chemistry, Visva-Bharati (a Central University), Santiniketan 731235, West Bengal, India;2. MedChem Herbal Research Group, Faculty of Pharmacy, Universiti Teknologi MARA, 42300 Puncak Alam, Selangor, Malaysia;3. PLS Core, UiTM, 40450 Shah Alam, Malaysia;4. Drug Theoretics and Cheminformatics Laboratory, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India;5. Manchester Institute of Biotechnology, 131 Princess Street, Manchester M1 7DN, United Kingdom |
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| Abstract: | A simple, efficient and green approach for the synthesis of spiro-dihydropyridines derivatives by one-pot multi-component reaction of isatin or acenaphthoquinone derivatives (1 equiv) with malononitrile (1 equiv) and N,N′-substituted-2-nitroethene-1,1-diamines (1 equiv) in PEG-400 under catalyst-free conditions is described. This method provides several advantages such as environmental friendliness, short reaction time, and simple workup procedure for the synthesis of biologically important compounds. The ability of synthesized compounds in inhibition of acetyl and butyrylcholinesterase were investigated both in vitro and in silico. All compounds showed moderate to high level activity against both acetyl and butyrylcholinesterase. There was a good correlation between in vitro and in silico studies. |
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| Keywords: | Spiro-dihydropyridines Multi-component reactions Catalyst-free Acetylcholinesterase inhibition Butyrylcholinesterase inhibition |
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