Back to Search
Start Over
Dicyanoanilines as potential and dual inhibitors of α-amylase and α-glucosidase enzymes: Synthesis, characterization, in vitro, in silico, and kinetics studies
- Source :
- Arabian Journal of Chemistry, Vol 15, Iss 3, Pp 103651- (2022)
- Publication Year :
- 2022
- Publisher :
- Elsevier, 2022.
-
Abstract
- The present study comprised of the synthesis of dicyanoaniline derivatives of pyridine, thiophene, furan, and substituted phenyl 1–29. All synthetic derivatives were evaluated for their potential to inhibit α-amylase and α-glucosidase enzymes. The synthesized compounds are classified into three categories A, B, and C based on variable substituents at R1 and R2, and the structure–activity relationship was discussed accordingly. Amongst twenty-nine derivatives, 1–29, five compounds 2, 9, 18, 23, and 24 displayed excellent inhibition against α-amylase and α-glucosidase enzymes with the IC50 values ranging between 20.33 ± 0.02–25.50 ± 0.06 µM and 21.01 ± 0.12–27.75 ± 0.17 µM, respectively, while other compounds showed moderate to weak inhibition against both enzymes. Acarbose was used as the positive control in this study. The enzyme kinetic studies showed non-competitive and un-competitive types of inhibition mechanism against α-amylase and α-glucosidase enzymes, respectively. In silico studies have demonstrated the involvement of these molecules in numerous binding interactions within the active site of the enzyme.
Details
- Language :
- English
- ISSN :
- 18785352
- Volume :
- 15
- Issue :
- 3
- Database :
- Directory of Open Access Journals
- Journal :
- Arabian Journal of Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.85b9a47301b04eb5a855757f22723039
- Document Type :
- article
- Full Text :
- https://doi.org/10.1016/j.arabjc.2021.103651