This manuscript describes the design and synthesis of a series of diverse N-Acyl Anthranilamides and quinazolin-4-ones derivatives (3a-3n, and 4a-4d) inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia. A series of N-Acyl Anthranilamides and quinazolin-4-ones derivatives (3a-3n, and 4a-4d) were synthesized and their chemical structures were confirmed by 1 H, 13C NMR and mass spectral data. Analogs were optimized using structure-based design and physical property considerations resulting in the identification of 4b and 3d, a hepatoselective HMG-CoA reductase inhibitor with excellent acute and chronic efficacy in a vitro model.
Ismail, P. S., Khan, I., Kumar, V., Verma, V. P., Shukla, M., Dhasmana, A., Pandey, S., Singh, G. P., Singh, J., & Khan, S. (2019). Facile synthesis of diverse N-Acyl Anthranilamides and quinazolin-4-ones as HMG-CoA reductase inhibitor via Pd-catalyzed cascade reaction. Chemistry & Biology Interface, 9(3), 172–185.
Chemistry & Biology Interface
Immunology and Microbiology