Acetylcholinesterase inhibitory potency of new pyrazoline derivative

TUĞRAK M., GÜL H. İ., GÜLÇİN İ.

JOURNAL OF RESEARCH IN PHARMACY, cilt.24, sa.4, ss.464-471, 2020 (ESCI) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 24 Sayı: 4
  • Basım Tarihi: 2020
  • Doi Numarası: 10.35333/jrp.2020.194
  • Dergi Adı: JOURNAL OF RESEARCH IN PHARMACY
  • Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
  • Sayfa Sayıları: ss.464-471
  • Anahtar Kelimeler: Acetylcholinesterase, alzheimer disease, benzothiazol, pyrazoline, SELECTIVE MONOAMINE-OXIDASE, BIOLOGICAL EVALUATION, ANTIFUNGAL ACTIVITY, MOLECULAR DOCKING, B INHIBITORS, CHALCONES, 3D-QSAR, DISEASE
  • Atatürk Üniversitesi Adresli: Evet

Özet

Alzheimer's disease (AD) has no current cure and its mechanism is not fully known, but treatments for symptoms are available. Acetylcholinesterase (AChE) has been reported to be an applicable therapeutic target in patient with AD. Acetylcholinesterase inhibitors (AChEIs) are commonly used for it. For this purpose, novel series of pyrazoline based compounds [2-(3-(4-methoxypheny0-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole,1-9] were synthesized and AChE inhibitory potencies were reported here. The results indicated that compound 1 (Ki= 0.13 +/- 0.004 mu M) possessed the highest AChE inhibitory effect in series, which is two times more potent than the reference compound Tacrin (Ki= 0.26 +/- 0.045 mu M). So, pyrazoline derivative 1 can be considered as a lead inhibitor in designing new AChE inhibitors.