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

ÖZDEMİR Z., Alagoz M. A., Uslu H., KARAKURT A., Erikci A., Ucar G., ...Daha Fazla

PHARMACOLOGICAL REPORTS, cilt.72, sa.3, ss.692-704, 2020 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 72 Sayı: 3
  • Basım Tarihi: 2020
  • Doi Numarası: 10.1007/s43440-020-00070-w
  • Dergi Adı: PHARMACOLOGICAL REPORTS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, EMBASE, MEDLINE
  • Sayfa Sayıları: ss.692-704
  • Anahtar Kelimeler: Pyridazinone, Monoamine oxidase inhibition, Molecular docking, ACCURATE DOCKING, DESIGN, GLIDE, ACETYLCHOLINESTERASE, 3(2H)-PYRIDAZINONE, PROGRAM
  • İnönü Üniversitesi Adresli: Evet

Özet

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.