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Synthesis of New Valinol‐Derived Sultam Triazoles as α‐Glucosidase Inhibitors.

Authors :
Jaffery, Syeda Mehak Fatima
Khan, Maria Aqeel
Ullah, Saeed
Atia‐tul‐Wahab
Choudhary, Muhammad Iqbal
Basha, Fatima Zehra
Source :
ChemistrySelect. 10/6/2021, Vol. 6 Issue 37, p9780-9786. 7p.
Publication Year :
2021

Abstract

α‐Glucosidase inhibition is one of the key targets for controlling diabetes. In consideration of that, new L‐valinol derived fluorinated sultam triazoles were synthesized as α‐glucosidase inhibitors, and their activities were further compared with the precursor molecules (sulfonamides, sultams, and N‐propargyl sultams). Primarily, all the synthesized sultam triazoles and precursor compounds (sulfonamides, sultams, and N‐propargyl sultams) were evaluated for different biological activities, including cytotoxicity, anti‐inflammatory, and α‐glucosidase inhibitory activities. Results revealed that only sultam triazoles exhibited inhibition against α‐glucosidase enzyme (IC50 values: 173 to 194 μM) using acarbose (IC50: 875.85 ± 2.03 μM) as the standard drug. These sultam triazoles were prepared after few steps, starting from enantiopure L‐valinol, which differ electronically (due to the position of fluorine atom and different positions on aromatic ring). Structures of all the compounds were evaluated using different spectroscopic techniques. Kinetics of active compounds were also investigated to find their mode of inhibition. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
23656549
Volume :
6
Issue :
37
Database :
Academic Search Index
Journal :
ChemistrySelect
Publication Type :
Academic Journal
Accession number :
152886513
Full Text :
https://doi.org/10.1002/slct.202102119