A new series of pyridazinone derivatives as cholinesterases inhibitors: Synthesis, in vitro activity and molecular modeling studies


ÖZÇELİK A. B. , ÖZDEMİR Z. , SARI S., UTKU S., UYSAL M.

PHARMACOLOGICAL REPORTS, cilt.71, ss.1253-1263, 2019 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 71 Konu: 6
  • Basım Tarihi: 2019
  • Doi Numarası: 10.1016/j.pharep.2019.07.006
  • Dergi Adı: PHARMACOLOGICAL REPORTS
  • Sayfa Sayıları: ss.1253-1263

Özet

Background: The pyridazinone nucleus has been incorporated into a wide variety of therapeutically interesting molecules to transform them into better drugs. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known to be serine hydrolase enzymes responsible for the hydrolysis of acetylcholine (ACh). Inhibition of cholinesterases is an effective method to curb Alzheimer's disease. Here, we prepared 12 new 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(nonsubstituted/4-substituted benzenesulfonohydrazide) derivatives and evaluated their inhibitory effects on AChE/BChE in pursuit of potent dual inhibitors for Alzheirmer's Disease. We also tried to get insights into binding interactions of the synthesized compounds in the active site of both enzymes by using molecular docking approach.