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Yaghoub Sarrafi

Yaghoub Sarrafi

Academic rank: Professor
ORCID:
Education: PhD.
ScopusId:
Faculty: Faculty of Chemistry
Address:
Phone: 9121978350

Research

Title
New tacrin e-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-p henyl-4 H -pyrano[2,3- b ]quinoline -3-carboxylates
Type
JournalPaper
Keywords
Acetylcholinesterase, Butyrylcholinesterase, Alzheimer's disease, Tacrine
Year
2017
Journal EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
DOI
Researchers Mohammad Eghtedari ، Yaghoub Sarrafi ، Hamid Nadri ، Mohammad Mahdavi ، Alireza Moradi ، Farshad Homayouni Moghadam ، Saeed Emami ، Loghman Firoozpour ، Ali Asadipour ، Omid Sabzevari ، Alireza Foroumadi

Abstract

A series of poly-functionalized tacrine-derived compounds namely 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates were designed and synthesized as cholinesterases inhibitors. The in vitro inhibition assay against AChE and BuChE demonstrated that most of compounds had potent AChE inhibitory with reserving potential of BuChE inhibition. Among them, compound 6i bearing a 4-(3-bromophenyl) moiety showed the most potent activity against AChE/BuChE (IC50s values of 0.069 and 1.35 μM, respectively). The anti-AChE activity of 6i was five times more than that of tacrine. The SAR study revealed that chloro/bromo substituent at ortho or meta position of the 4-phenyl ring can improve the anticholinesterase activity.