Startseite New indane derivatives containing 2-hydrazinothiazole as potential acetylcholinesterase and monoamine oxidase-B inhibitors
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New indane derivatives containing 2-hydrazinothiazole as potential acetylcholinesterase and monoamine oxidase-B inhibitors

  • İsmail Okan Ateş , Asaf Evrim Evren ORCID logo , Begüm Nurpelin Sağlik und Leyla Yurttaş EMAIL logo
Veröffentlicht/Copyright: 28. Mai 2021
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Zeitschrift für Naturforschung C
Aus der Zeitschrift Zeitschrift für Naturforschung C Band 76 Heft 9-10

Abstract

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.

Keywords: ADME prediction; anticholinesterase activity; indane; monoamine oxidase inhibition; thiazole
Corresponding author: Leyla Yurttaş, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey, E-mail:

Acknowledgments

We gratefully thank Anadolu University DOPNA Laboratory for analyzing the synthesized compounds.

  1. Author contributions: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.

  2. Research funding: None declared.

  3. Conflict of interest statement: The authors confirm that this article content has no conflict of interest.

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Supplementary material

The online version of this article offers supplementary material (https://doi.org/10.1515/znc-2021-0058).

Received: 2021-02-26
Accepted: 2021-05-08
Published Online: 2021-05-28
Published in Print: 2021-09-27

© 2021 Walter de Gruyter GmbH, Berlin/Boston

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https://doi.org/10.1515/znc-2021-0058
Schlagwörter für diesen Artikel
ADME prediction; anticholinesterase activity; indane; monoamine oxidase inhibition; thiazole

Artikel in diesem Heft

  1. Frontmatter
  2. Review Article
  3. A review on chemistry, source and therapeutic potential of lambertianic acid
  4. Research Articles
  5. Neuroprotective constituents of Actaea acuminata (Wall. ex Royle) H. Hara roots
  6. Receptor-mediated biological effects of extracts obtained from three Asplenium species
  7. Evaluation of biological activities of Barbarea integrifolia and isolation of a new glucosinolate derivated compound
  8. Comparative spasmolytic effect between Cinnamomum tamala and Cinnamomum verum leaf essential oils and eugenol through in vitro and in silico approaches
  9. Simple mathematical models for controlling COVID-19 transmission through social distancing and community awareness
  10. Benzylisoquinoline alkaloids from Nelumbo nucifera Gaertn. petals with antiausterity activities against the HeLa human cervical cancer cell line
  11. Cardioprotective effects of omega 3 fatty acids from fish oil and it enhances autoimmunity in porcine cardiac myosin-induced myocarditis in the rat model
  12. New indane derivatives containing 2-hydrazinothiazole as potential acetylcholinesterase and monoamine oxidase-B inhibitors
  13. Rapid communication
  14. Seroprevalence of SARS-CoV-2 in Pakistan: an update on epidemiological trends
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