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, Pathan Sultan; Khan, Irfan; Kumar, Vivek; Verma, Ved Prakash; Shukla, Monika; Dhasmana, Anupam; Pandey, Shashi; Singh, Girdhar Pal; Singh, Jaybir; and Khan, Shahnawaz, "Facile synthesis of diverse N-Acyl Anthranilamides and quinazolin-4-ones as HMG-CoA reductase inhibitor via Pd-catalyzed cascade reaction" (2019). School of Medicine Publications and Presentations. 148.
Chemistry & Biology Interface
Immunology and Microbiology