{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Shahid Nadeem M"],"funding":["King Abdulaziz University"],"pagination":["9369-9379"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8945123"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["7(11)"],"pubmed_abstract":["In continuation of our previous study to identify multitarget inhibitors of cholinesterases (ChEs) and monoamine oxidase (MAOs) isoforms, we synthesized and evaluated 2-arylidine derivatives of thiazolopyrimidine for the treatment of Alzheimer disease. Three series of compounds with different linker size and target-anchoring functional groups were synthesized. Compounds <b>34</b>-<b>37</b> showed excellent to good AChE and BChE inhibition potential at nanomolar to low micromolar concentration. While all the compounds showed excellent MAO-B inhibition and selectivity relative to MAO-A, compounds <b>25</b> and <b>36</b> emerged as the most potent MAO-B inhibitors of all the series of synthesized compounds with IC<sub>50</sub> values of 0.13 μM and 0.10 μM, respectively. Furthermore, kinetic "],"journal":["ACS omega"],"pubmed_title":["Design, Synthesis, and Bioevaluation of Indole Core Containing 2-Arylidine Derivatives of Thiazolopyrimidine as Multitarget Inhibitors of Cholinesterases and Monoamine Oxidase A/B for the Treatment of Alzheimer Disease."],"pmcid":["PMC8945123"],"funding_grant_id":["KEP-7-130-42"],"pubmed_authors":["Rashid U","Shahid Nadeem M","Azam Khan J","Kazmi I"],"additional_accession":[]},"is_claimable":false,"name":"Design, Synthesis, and Bioevaluation of Indole Core Containing 2-Arylidine Derivatives of Thiazolopyrimidine as Multitarget Inhibitors of Cholinesterases and Monoamine Oxidase A/B for the Treatment of Alzheimer Disease.","description":"In continuation of our previous study to identify multitarget inhibitors of cholinesterases (ChEs) and monoamine oxidase (MAOs) isoforms, we synthesized and evaluated 2-arylidine derivatives of thiazolopyrimidine for the treatment of Alzheimer disease. Three series of compounds with different linker size and target-anchoring functional groups were synthesized. Compounds <b>34</b>-<b>37</b> showed excellent to good AChE and BChE inhibition potential at nanomolar to low micromolar concentration. While all the compounds showed excellent MAO-B inhibition and selectivity relative to MAO-A, compounds <b>25</b> and <b>36</b> emerged as the most potent MAO-B inhibitors of all the series of synthesized compounds with IC<sub>50</sub> values of 0.13 μM and 0.10 μM, respectively. Furthermore, kinetic ","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Mar","modification":"2026-05-30T20:57:55.313Z","creation":"2025-04-04T10:02:32.947Z"},"accession":"S-EPMC8945123","cross_references":{"pubmed":["35350344"],"doi":["10.1021/acsomega.1c06344"]}}