Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease

Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease

A series of thirty (30) thiazole analogs were prepared, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinesterase inhibitory activity with IC50 value ranging between 1.59 ± 0.01...

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Published in:Bioorganic Chemistry
Main Author: Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
Format: Article
Language:English
Published: Academic Press Inc. 2015
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84940020718&doi=10.1016%2fj.bioorg.2015.08.002&partnerID=40&md5=7105aa5a0971138a2feb2a54448372d9
id 2-s2.0-84940020718
spelling 2-s2.0-84940020718
Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
2015
Bioorganic Chemistry
62

10.1016/j.bioorg.2015.08.002
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84940020718&doi=10.1016%2fj.bioorg.2015.08.002&partnerID=40&md5=7105aa5a0971138a2feb2a54448372d9
A series of thirty (30) thiazole analogs were prepared, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinesterase inhibitory activity with IC50 value ranging between 1.59 ± 0.01 and 389.25 ± 1.75 μM when compared with the standard eserine (IC50, 0.85 ± 0.0001 μM). Analogs 15, 7, 12, 9, 14, 1, 30 with IC50 values 1.59 ± 0.01, 1.77 ± 0.01, 6.21 ± 0.01, 7.56 ± 0.01, 8.46 ± 0.01, 14.81 ± 0.32 and 16.54 ± 0.21 μM respectively showed excellent inhibitory potential. Seven analogs 15, 20, 19, 24, 28, 30 and 25 exhibited good acetylcholinesterase inhibitory potential with IC50 values 21.3 ± 0.50, 35.3 ± 0.64, 36.6 ± 0.70, 44.81 ± 0.81, 46.36 ± 0.84, 48.2 ± 0.06 and 48.72 ± 0.91 μM respectively. All other analogs also exhibited well to moderate enzyme inhibition. The binding mode of these compounds was confirmed through molecular docking. © 2015 Elsevier Inc. All rights reserved.
Academic Press Inc.
452068
English
Article
author Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
spellingShingle Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
author_facet Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
author_sort Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
title Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
title_short Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
title_full Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
title_fullStr Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
title_full_unstemmed Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
title_sort Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
publishDate 2015
container_title Bioorganic Chemistry
container_volume 62
container_issue
doi_str_mv 10.1016/j.bioorg.2015.08.002
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84940020718&doi=10.1016%2fj.bioorg.2015.08.002&partnerID=40&md5=7105aa5a0971138a2feb2a54448372d9
description A series of thirty (30) thiazole analogs were prepared, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinesterase inhibitory activity with IC50 value ranging between 1.59 ± 0.01 and 389.25 ± 1.75 μM when compared with the standard eserine (IC50, 0.85 ± 0.0001 μM). Analogs 15, 7, 12, 9, 14, 1, 30 with IC50 values 1.59 ± 0.01, 1.77 ± 0.01, 6.21 ± 0.01, 7.56 ± 0.01, 8.46 ± 0.01, 14.81 ± 0.32 and 16.54 ± 0.21 μM respectively showed excellent inhibitory potential. Seven analogs 15, 20, 19, 24, 28, 30 and 25 exhibited good acetylcholinesterase inhibitory potential with IC50 values 21.3 ± 0.50, 35.3 ± 0.64, 36.6 ± 0.70, 44.81 ± 0.81, 46.36 ± 0.84, 48.2 ± 0.06 and 48.72 ± 0.91 μM respectively. All other analogs also exhibited well to moderate enzyme inhibition. The binding mode of these compounds was confirmed through molecular docking. © 2015 Elsevier Inc. All rights reserved.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
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