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Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series o...
| Autores principales: | , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Bentham Science Publishers Ltd
2014
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3977535/ https://www.ncbi.nlm.nih.gov/pubmed/24719609 http://dx.doi.org/10.2174/15701808113106660078 |
| _version_ | 1782310435955933184 |
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| author | Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir |
| author_facet | Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir |
| author_sort | Yar, Muhammad |
| collection | PubMed |
| description | Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC(50) 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC(50) 55.21±0.12 μM). |
| format | Online Article Text |
| id | pubmed-3977535 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| publisher | Bentham Science Publishers Ltd |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-39775352014-04-07 Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir Lett Drug Des Discov Article Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC(50) 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC(50) 55.21±0.12 μM). Bentham Science Publishers Ltd 2014-03 2014-03 /pmc/articles/PMC3977535/ /pubmed/24719609 http://dx.doi.org/10.2174/15701808113106660078 Text en © 2014 Bentham Science Publishers Ltd. http://creativecommons.org/licenses/by/2.5/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.5/), which permits unrestrictive use, distribution, and reproduction in any medium, provided the original work is properly cited. |
| spellingShingle | Article Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking |
| title | Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors:
in vitro Inhibition Studies with in silico Docking |
| title_full | Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors:
in vitro Inhibition Studies with in silico Docking |
| title_fullStr | Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors:
in vitro Inhibition Studies with in silico Docking |
| title_full_unstemmed | Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors:
in vitro Inhibition Studies with in silico Docking |
| title_short | Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors:
in vitro Inhibition Studies with in silico Docking |
| title_sort | design and synthesis of new dual binding site cholinesterase inhibitors:
in vitro inhibition studies with in silico docking |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3977535/ https://www.ncbi.nlm.nih.gov/pubmed/24719609 http://dx.doi.org/10.2174/15701808113106660078 |
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