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oai:ebyu-rdlopen.rawdatalibrary.net:ebyu/131552026-10-18T20:43:17Zopenairedrivercom_ebyu_10000col_ebyu_10001

Phenothiazine-based chalcones as potential dual-target inhibitors toward cholinesterases (AChE, BuChE) and monoamine oxidases (MAO-A, MAO-B)Yamali, CemEngin, Feyza SenaBilginer, SinanTugrak, MehtapOzmen Ozgun, DilanOzli, GulsenLevent, SerkanSaglik, Begum NurpelinOzkay, YusufGul, Halise Inci1 (10h phenothiazin 2 yl) 3 aryl 2 propen 1 one derivative1 (10h phenothiazine 2 yl) 3 (2 fluorophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (2,4 dichlorophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (3 bromophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (3 fluorophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (3 nitrophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (3,4 dichlorophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (3,4 methylenedioxyphenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 benzyloxyphenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 chlorophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 fluorophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 methoxyphenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 methylphenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 nitrophenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (4 trifluoromethylphenyl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 (thiophene 2 yl)prop 2 en 1 one1 (10h phenothiazine 2 yl) 3 phenyl prop 2 en 1 oneacetylcholinesteraseamine oxidase (flavin containing) isoenzyme Aamine oxidase (flavin containing) isoenzyme Bchalcone derivativecholinesteraseclorgylinedonepezilphenothiazine derivativeselegilinetacrineunclassified drugAlzheimer diseaseArticleChalcones targeting neurodegenerative diseases have been known as attractive structures in drug design and discovery. In this study, phenothiazine-based chalcones as ChEs and MAOs inhibitors were designed and synthesized via base-catalyzed Claisen-Schmidt condensation, and chemical structures of the compounds were elucidated by NMRs and HRMS. Compounds 3 and 9 showed promising inhibition potency against AChE enzyme with IC50 values of 0.221 μM and 0.053 μM while compound 9 displayed remarkable inhibition potency toward MAO-B enzyme with IC50 value of 0.048 μM. Compound 9, as a dual-target inhibitor, selectively inhibited AChE and MAO-B enzymes. This promising behavior is an advantage for the compound since MAO-B and AChE inhibition have a role in Alzheimer's disease. Fused tricyclic ring systems such as phenothiazine incorporated with chalcone moiety being multitargeting ligands may help scientists for the rational design of novel lead compounds targeting neurodegenerative illnesses. © 2020 Wiley Periodicals LLC.HeteroCorporation2021Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/13155https://doi.org/10.1002/jhet.41560022-152XenJournal of Heterocyclic Chemistryinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/13155