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

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

Mirzazadeh R¹ ; Asgari MS² ; Barzegari E³ ; Pedrood K⁴ ; Mohammadikhanaposhtani M⁵ ; Sherafati M⁴ ; Larijani B⁴ ; Rastegar H⁶ ; Rahmani H⁷ ; Mahdavi M⁴ ; Taslimi P⁸ ; Eda M UC⁹ ; Gulcin I⁹

Show Affiliations

1. Department of Biochemistry, Pasteur Institute of Iran, Tehran, Iran
2. Department of Chemistry, Iran University of Science and Technology, Tehran, Iran
3. Medical Biology Research Center, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran
4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
5. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
6. Cosmetic Products Research Center, Iranian Food and Drug Administration, MOHE, Tehran, Iran
7. Department of Health Management and Economics, School of Public Health, Tehran University of Medical Sciences, Tehran, Iran
8. Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
9. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey

Source: Archiv der Pharmazie Published:2021

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. © 2021 Deutsche Pharmazeutische Gesellschaft

Style	Citing Format
MLA	Mirzazadeh R, et al.. "New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies." Archiv der Pharmazie, vol. 354, no. 9, 2021, pp. -.
APA	Mirzazadeh R, Asgari MS, Barzegari E, Pedrood K, Mohammadikhanaposhtani M, Sherafati M, Larijani B, Rastegar H, Rahmani H, Mahdavi M, Taslimi P, Eda M UC, Gulcin I (2021). New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies. Archiv der Pharmazie, 354(9), -.
Chicago	Mirzazadeh R, Asgari MS, Barzegari E, Pedrood K, Mohammadikhanaposhtani M, Sherafati M, Larijani B, et al.. "New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies." Archiv der Pharmazie 354, no. 9 (2021): -.
Harvard	Mirzazadeh R et al. (2021) 'New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies', Archiv der Pharmazie, 354(9), pp. -.
Vancouver	Mirzazadeh R, Asgari MS, Barzegari E, Pedrood K, Mohammadikhanaposhtani M, Sherafati M, et al.. New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies. Archiv der Pharmazie. 2021;354(9):-.
BibTex	@article{ author = {Mirzazadeh R and Asgari MS and Barzegari E and Pedrood K and Mohammadikhanaposhtani M and Sherafati M and Larijani B and Rastegar H and Rahmani H and Mahdavi M and Taslimi P and Eda M UC and Gulcin I}, title = {New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies}, journal = {Archiv der Pharmazie}, volume = {354}, number = {9}, pages = {-}, year = {2021} }
RIS	TY - JOUR AU - Mirzazadeh R AU - Asgari MS AU - Barzegari E AU - Pedrood K AU - Mohammadikhanaposhtani M AU - Sherafati M AU - Larijani B AU - Rastegar H AU - Rahmani H AU - Mahdavi M AU - Taslimi P AU - Eda M UC AU - Gulcin I TI - New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies JO - Archiv der Pharmazie VL - 354 IS - 9 SP - EP - PY - 2021 ER -

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