Synthesis and molecular modeling studies of cholinesterase inhibitor dispiro[indoline-3,2'-pyrrolidine-3',3''-pyrrolidines].
| Autor: | Youssef MA; Department of Chemistry, Faculty of Science, Helwan University Helwan Egypt., Panda SS; Department of Chemistry and Physics, Augusta University Augusta GA 30912 USA., El-Shiekh RA; Department of Pharmacognosy, Faculty of Pharmacy, Cairo University Cairo 11562 Egypt., Shalaby EM; X-Ray Crystallography Lab., Physics Division, National Research Centre Dokki Giza 12622 Egypt., Aboshouk DR; Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com., Fayad W; Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre Dokki Giza 12622 Egypt., Fawzy NG; Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com., Girgis AS; Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com. |
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| Jazyk: | angličtina |
| Zdroj: | RSC advances [RSC Adv] 2020 Jun 08; Vol. 10 (37), pp. 21830-21838. Date of Electronic Publication: 2020 Jun 08 (Print Publication: 2020). |
| DOI: | 10.1039/d0ra03064c |
| Abstrakt: | A set of dispiro[indoline-3,2'-pyrrolidine-3',3''-pyrrolidines] 8a-l was regioselectively synthesized utilizing multi-component azomethine cycloaddition reaction of 3-(arylmethylidene)pyrrolidine-2,5-diones 5a-e, isatins 6a-c and sarcosine 7. Single crystal X-ray studies of 8c add conclusive support for the structure. Compounds 8e and 8g reveal cholinesterase inhibitory properties with promising efficacy against both AChE and BChE and were found to be more selective towards AChE than BChE as indicted by the selectivity index like Donepezil (a clinically used cholinesterase inhibitory drug). Molecular modeling studies assist in understanding the bio-observations and identifying the responsible parameters behind biological properties. Competing Interests: There is no conflict to declare. (This journal is © The Royal Society of Chemistry.) |
| Databáze: | MEDLINE |
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