Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular modeling studies of imidazo[2,1-b]thiazole derivatives bearing thiosemicarbazide moiety

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Dincel E. D., Hasbal Çelikok G., Yılmaz Özden T., Ulusoy-Güzeldemirci N.

Journal of Research in Pharmacy, vol.28, no.1, pp.155-163, 2024 (ESCI, Scopus, TRDizin) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 28 Issue: 1
  • Publication Date: 2024
  • Doi Number: 10.29228/jrp.684
  • Journal Name: Journal of Research in Pharmacy
  • Journal Indexes: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.155-163
  • Keywords: acetylcholinesterase, biological evaluation, molecular modeling, Synthesis
  • Open Archive Collection: AVESIS Open Access Collection
  • Istanbul University Affiliated: Yes

Abstract

Herein, we report the in vitro Acetylcholinesterase (AChE) inhibitory activities of imidazo[2,1-b]thiazole derivatives bearing thiosemicarbazide moiety. The compounds were characterized by diverse spectral methods and reported by our research team previously. As a novelty we conducted in vitro AChE inhibitory activities of the title compounds and performed in silico studies to provide insight related to activity mechanism of the compounds. Compound 4f displayed the best biological activity within our compounds with 69.92% enzyme inhibition value (at a final concentration of 0.08 mg/mL) and 0.0245 mg/mL IC50 value.