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Title: Design and Synthesis of Some Arylhydrazone Derivatives as Potential Faah Inhibitors
Other Titles: Potansiyel Faah İnhibitörü Olarak Bazı Arilhidrazon Türevi Bileşiklerin Tasarımı ve Sentezi
Authors: Gür, Maz, T.
Turanlı, S.
Çalışkan, H.B.
Keywords: Arylhydrazones
arylhydrazone derivative
fatty acid amidase inhibitor
n (3 pyridazinyl) 4 [3 (5 trifluoromethyl 2 pyridinyloxy)benzylidene] 1 piperidinecarboxamide
n' [(4 phenoxyphenyl)methylidene]pyridine 3 carbohydrazide
n' [[ 4 (pyridin 2 yloxy)phenyl]methylidene]pyridine 3 carbohydrazide
n' [[4 (benzyloxy)phenyl]methylidene]pyridine 3 carbohydrazide
n' [[4 [(4 cyanophenyl)methoxy]phenyl]methylidene]pyridine 3 carbohydrazide
n' [[4 [(4 fluorophenyl)methoxy]phenyl]methylidene]benzohydrazide
n' [[4 [(4 fluorophenyl)methoxy]phenyl]methylidene]pyridine 3 carbohydrazide
n' [[4 [(4 methoxyphenyl)methoxy]phenyl]methylidene]pyridine 3 carbohydrazide
unclassified drug
carbon nuclear magnetic resonance
chemical structure
controlled study
drug design
drug synthesis
enzyme active site
enzyme inhibition
hydrogen bond
liquid chromatography-mass spectrometry
melting point
molecular docking
molecular model
proton nuclear magnetic resonance
X ray crystallography
Issue Date: 2023
Publisher: University of Ankara
Abstract: Objective: The aim was to design, synthesis and investigation of possible interactions in the enzyme active site of a series of arylhydrazone derivatives for the inhibition of the FAAH enzyme.” Material and Method: Arylhydrazone derivatives were obtained through the reaction of nicotinic hydrazide or benzohydrazide with appropriate aldehyde derivatives, and the obtained crude product was recrystallized from ethanol. After elucidating chemical structures of the compounds via spectroscopic methods, the inhibitory activities against hFAAH were screened. The results were further supported with molecular modeling studies. Result and Discussion: In this study, a new series of seven arylhydrazone derivatives were screened against hFAAH. 4-phenoxyphenyl bearing derivative 5 was found to inhibit hFAAH 40 % at 10 µM which indicates that newly developed inhibitor could serve as a starting point for improving inhibitory effect of the new series. © 2023 University of Ankara. All rights reserved.
ISSN: 2564-6524
Appears in Collections:Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection

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