| Title : New quinoxalin-1,3,4-oxadiazole derivatives: Synthesis, characterization, in vitro biological evaluations, and molecular modeling studies - Mirzazadeh_2021_Arch.Pharm.(Weinheim)__e2000471 |
| Author(s) : Mirzazadeh R , Asgari MS , Barzegari E , Pedrood K , Mohammadi-Khanaposhtani M , Sherafati M , Larijani B , Rastegar H , Rahmani H , Mahdavi M , Taslimi P , Uc EM , Gulcin I |
| Ref : Arch Pharm (Weinheim) , :e2000471 , 2021 |
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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 alpha-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 alpha-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. |
| PubMedSearch : Mirzazadeh_2021_Arch.Pharm.(Weinheim)__e2000471 |
| PubMedID: 33999440 |
Mirzazadeh R, Asgari MS, Barzegari E, Pedrood K, Mohammadi-Khanaposhtani M, Sherafati M, Larijani B, Rastegar H, Rahmani H, Mahdavi M, Taslimi P, Uc EM, Gulcin I (2021)
New quinoxalin-1,3,4-oxadiazole derivatives: Synthesis, characterization, in vitro biological evaluations, and molecular modeling studies
Arch Pharm (Weinheim)
:e2000471
Mirzazadeh R, Asgari MS, Barzegari E, Pedrood K, Mohammadi-Khanaposhtani M, Sherafati M, Larijani B, Rastegar H, Rahmani H, Mahdavi M, Taslimi P, Uc EM, Gulcin I (2021)
Arch Pharm (Weinheim)
:e2000471