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

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DİNCEL E. D., HASBAL ÇELİKOK G., YILMAZ ÖZDEN T., Ulusoy-Güzeldemirci N.

Journal of Research in Pharmacy, cilt.28, sa.1, ss.155-163, 2024 (ESCI) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 28 Sayı: 1
  • Basım Tarihi: 2024
  • Doi Numarası: 10.29228/jrp.684
  • Dergi Adı: Journal of Research in Pharmacy
  • Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
  • Sayfa Sayıları: ss.155-163
  • Anahtar Kelimeler: acetylcholinesterase, biological evaluation, molecular modeling, Synthesis
  • İstanbul Üniversitesi Adresli: Evet

Özet

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.