New Quinoxalin-1,3,4-oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies

Roghieh Mirzazadeh,Mohammad S. Asgari,Ebrahim Barzegari,Keyvan Pedrood,Maryam Mohammadi-Khanaposhtani,Maedeh Sherafati,Bagher Larijani,Hossein Rastegar,Hojjat Rahmani,Mohammad Mahdavi,Parham Taslimi,Eda M. Uc,Ilhami Gulcin

Archiv Der Pharmazie（2021）SCI 4区SCI 3区

Cited 13|Views1

Abstract

A new series of quinoxalin-1,3,4-oxadiazole (10a-l) derivatives was synthesized and evaluated against some metabolic enzymes including human carbonic anhydrase (hCA) isoenzymes I and II (carbonic anhydrases I and II), cholinesterase (acetylcholinesterase and butyrylcholinesterase), and α-glucosidase. Obtained data revealed that all the synthesized compounds were more potent as compared with the used standard inhibitors against studied target enzymes. Among the synthesized compounds, 4-fluoro derivative (10f) against hCA I, 4-chloro derivative (10i) against hCA II, 3-fluoro derivative (10e) against acetylcholinesterase and butyrylcholinesterase, and 3-bromo derivative (10k) against α-glucosidase were the most potent compounds with inhibitory activity around 1.8- to 7.37-fold better than standard inhibitors. Furthermore, docking studies of these compounds were performed at the active site of their target enzymes.

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Key words

1,3,4-oxadiazole,carbonic anhydrase,cholinesterase,quinoxalin,alpha-glucosidase

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