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- Title
Microwave-assisted SiO<sub>2</sub>-H<sub>2</sub>SO<sub>4</sub>-catalyzed Synthesis of 3,4,6,7-Tetrahydro-3,3,6,6-tetramethyl-9,10- diphenylacridine-1,8-dione Derivatives as Cholesterol Esterase Inhibitors.
- Authors
SINGH, H.; SINGH, A.; GUPTA, M. K.; SHARMA, S.; BEDI, P. M. S.
- Abstract
A library of 3,4,6,7-tetrahydro-3,3,6,6-tetramethyl-9,10-diphenylacridine-1,8-dione derivatives were synthesized via microwave-assisted three-component reaction employing silica supported sulphuric acid under solvent free conditions and tested for in vitro cholesterol esterase inhibitory activity. All synthesized compounds exhibited moderate to good inhibition of cholesterol esterase enzyme. Among all the synthesized acridinedione derivatives, compound HSM-1a showed the most promising activity with IC50 value of 1.53 μM against cholesterol esterase enzyme. Enzyme kinetic studies carried out for HSM-1a, revealed its mixed-type inhibition approach. Molecular protein-ligand docking studies were also performed to figure out the key binding interactions of HSM-1a with the amino acid residues of the enzyme's active site. Furthermore, acquiescence of some potent compounds to the Lipinski rule was also determined.
- Subjects
SILICA; MICROWAVES; CATALYTIC activity; ACRIDINE derivatives; TETRAMETHYL compounds; CHOLESTEROL esterase; CHEMICAL synthesis; ENZYME inhibitors
- Publication
Indian Journal of Pharmaceutical Sciences, 2017, Vol 79, Issue 5, p801
- ISSN
0250-474X
- Publication type
Article
- DOI
10.4172/pharmaceutical-sciences.1000294