Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

Küçük Resim Yok

Tarih

2022

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Marmara Univ

Erişim Hakkı

info:eu-repo/semantics/openAccess

Özet

Alzheimer's disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 3(2H)pyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants (Ki) of the compounds against the AChE enzyme ranged from 2.35 +/- 0.18 to 5.15 +/- 0.46 mu M. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35 +/- 0.18 mu M. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure (PDB ID:4M0E).

Açıklama

Anahtar Kelimeler

Acetylcholinesterase, alzheimer's disease, molecular docking, pyridazinone, triazole

Kaynak

Journal of Research in Pharmacy

WoS Q Değeri

N/A

Scopus Q Değeri

Q3

Cilt

26

Sayı

5

Künye