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New indane derivatives containing 2-hydrazinothiazole as potential acetylcholinesterase and monoamine oxidase-B inhibitors.
Ates, Ismail Okan; Evren, Asaf Evrim; Saglik, Begüm Nurpelin; Yurttas, Leyla.
Afiliación
  • Ates IO; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey.
  • Evren AE; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey.
  • Saglik BN; Vocational School of Health Services, Bilecik Seyh Edebali University, Bilecik, Turkey.
  • Yurttas L; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey.
Z Naturforsch C J Biosci ; 76(9-10): 417-424, 2021 Sep 27.
Article en En | MEDLINE | ID: mdl-34047146
Although radical treatment of Alzheimer's and Parkinson's disease is not possible yet, it is aimed to slow the course of the disease and increase the life quality of individuals with the drugs used in the clinic at the present time. Successful results have been achieved in the use of cholinesterase inhibitors and monoamine oxidase inhibitors together in these neurodegenerative diseases. In this study, indane ring which are in the structure of anticholinesterase effective molecules and 2-hydrazinothiazole structure whose inhibitory activities reported on monoamine oxidase-B (MAO-B) were combined; 4-(substituted phenyl)-2-[2-(3-phenyl-2,3-dihydro-1H-inden-1-ylidene) hydrazinyl]thiazole derivatives (3a-3i) were synthesized as dual inhibitors. The structures of the compounds were verified by IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy. When enzyme inhibition activities were evaluated, it was determined that the compounds 3a (42.33%) and 3d (42.39%) on acetylcholinesterase (AChE) enzyme; compounds 3g (75.42%) and 3h (60.33%) showed inhibition on MAO-B enzyme at most, at 10-3 M concentration.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiazoles / Inhibidores de la Colinesterasa / Monoaminooxidasa / Inhibidores de la Monoaminooxidasa Límite: Humans Idioma: En Revista: Z Naturforsch C J Biosci Año: 2021 Tipo del documento: Article País de afiliación: Turquía Pais de publicación: Alemania

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiazoles / Inhibidores de la Colinesterasa / Monoaminooxidasa / Inhibidores de la Monoaminooxidasa Límite: Humans Idioma: En Revista: Z Naturforsch C J Biosci Año: 2021 Tipo del documento: Article País de afiliación: Turquía Pais de publicación: Alemania