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- Title
Design and Synthesis of 2-Substitutedphenyl Benzo[D]Thiazole Derivatives and Their β-Amyloid Aggregation and Cholinesterase Inhibitory Activities.
- Authors
Zengin, Merve; Unsal-Tan, Oya; Küçükkılınç, Tuba Tüylü; Ayazgok, Beyza; Balkan, Ayla
- Abstract
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.
- Subjects
THIAZOLES; PIPERAZINE; THIAZOLE derivatives; ALZHEIMER'S disease; BUTYRYLCHOLINESTERASE; IMIDAZOLES
- Publication
Pharmaceutical Chemistry Journal, 2019, Vol 53, Issue 4, p322
- ISSN
0091-150X
- Publication type
Article
- DOI
10.1007/s11094-019-02000-4