Synthesis, molecular modelling and biological activity of some pyridazinone derivatives as selective human monoamine oxidase-B inhibitors


ÖZDEMİR Z., ALAGÖZ M. A. , USLU H., KARAKURT A., Erikci A., Ucar G., ...More

PHARMACOLOGICAL REPORTS, vol.72, no.3, pp.692-704, 2020 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 72 Issue: 3
  • Publication Date: 2020
  • Doi Number: 10.1007/s43440-020-00070-w
  • Title of Journal : PHARMACOLOGICAL REPORTS
  • Page Numbers: pp.692-704
  • Keywords: Pyridazinone, Monoamine oxidase inhibition, Molecular docking, ACCURATE DOCKING, DESIGN, GLIDE, ACETYLCHOLINESTERASE, 3(2H)-PYRIDAZINONE, PROGRAM

Abstract

Background Since brain neurotransmitter levels are associated with the pathology of various neurodegenerative diseases like Parkinson and Alzheimer, monoamineoxidase (MAO) plays a critical role in balancing these neurotransmitters in the brain. MAO isoforms appear as promising drug targets for the development of central nervous system agents. Pyridazinones have a broad array of biological activities. Here, six pyridazinone derivatives were synthesized and their human monoamine oxidase inhibitory activities were evaluated by molecular docking studies, in silico ADME prediction and in vitro biological screening tests.