Design and Synthesis of 2-Substitutedphenyl Benzo[D]Thiazole Derivatives and Their β-Amyloid Aggregation and Cholinesterase Inhibitory Activities

Autor:	Oya Unsal-Tan, Tuba Tüylü Küçükkılınç, Beyza Ayazgök, Ayla Balkan, Merve Zengin
Rok vydání:	2019
Předmět:	Pharmacology chemistry.chemical_classification biology 010405 organic chemistry Stereochemistry 01 natural sciences Acetylcholinesterase In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry.chemical_compound Piperazine chemistry Drug Discovery biology.protein Azole Cholinergic Thiazole Butyrylcholinesterase Cholinesterase
Zdroj:	Pharmaceutical Chemistry Journal. 53:322-328
ISSN:	1573-9031 0091-150X
DOI:	10.1007/s11094-019-02000-4
Popis:	The occurrence of amyloid-β (Aβ) and reduced cholinergic tranmission are two major hallmarks of Alzheimer’s disease (AD). Therefore, a series of new 2-phenylbenzo[d]thiazoles substituted with azole/piperazine moieties were designed, synthesized, and evaluated as potential dual inhibitors of Aβ aggregation and cholinesterase (ChE) activities. In vitro studies showed that compound 2m containing an imidazole ring strongly inhibited Aβ1–40 (49.2%) and Aβ1-42 aggregation (60.6%). All derivatives exhibited weak inhibitory activities against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Therefore, compound 2m may represent promising therapeutic option for inhibiting Aβ-mediated pathology in AD.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::b60ea35a5d11db241052d61319b0c50d https://doi.org/10.1007/s11094-019-02000-4 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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