Journal article
New quinoxalin-1,3,4-oxadiazole derivatives: Synthesis, characterization, in vitro biological evaluations, and molecular modeling studies
Arch Pharm, Vol.354(9), pp.1-12
01/09/2021
PMID: 33999440
Metrics
1 Record Views
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.
Details
- Title
- New quinoxalin-1,3,4-oxadiazole derivatives: Synthesis, characterization, in vitro biological evaluations, and molecular modeling studies
- Creators
- Roghieh Mirzazadeh - Pasteur Institute of IranMohammad S. Asgari - Iran University of Science and TechnologyEbrahim Barzegari - Kermanshah University of Medical SciencesKeyvan Pedrood - Tehran University of Medical SciencesMaryam Mohammadi-Khanaposhtani - Babol University of Medical SciencesMaedeh Sherafati - Tehran University of Medical SciencesBagher Larijani - Tehran University of Medical SciencesHossein Rastegar - Iran Nanohealth Committee Food and Drug OrganizationHojjat Rahmani - Tehran University of Medical SciencesMohammad Mahdavi - Tehran University of Medical SciencesParham Taslimi - Bartin UniversityEda M. Uc - Atatürk UniversityIlhami Gulcin - Atatürk University
- Publication Details
- Arch Pharm, Vol.354(9), pp.1-12
- Publisher
- Wiley
- Number of pages
- 12
- Identifiers
- 991013400557302368
- Copyright
- © 2021 Deutsche Pharmazeutische Gesellschaft
- Academic Unit
- Faculty of Health
- Language
- English
- Resource Type
- Journal article