All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.


Microwave-assisted SiO2-H2SO4-catalyzed Synthesis of 3,4,6,7-Tetrahydro-3,3,6,6-Tetramethyl-9,10-diphenylacridine-1,8-dione Derivatives as Cholesterol Esterase Inhibitors

Author(s): H. Singh, H. Singh, A. Singh, M. K. Gupta1, S. Sharma* and P. M. S. Bedi
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar-143005, School of Pharmacy, Lloyd Institute of Management and Technology, Greater Noida-201308, India

Correspondence Address:
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar-143005, India, E-mail:

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.

Full-Text | PDF

Google scholar citation report
Citations : 66710

Indian Journal of Pharmaceutical Sciences received 66710 citations as per google scholar report