Quinoline-3-carboxamide Derivatives as Potential Cholesteryl Ester Transfer Protein Inhibitors

Abstract

A series of novel quinoline-3-carboxamide derivatives 10-17 and 23-27 were designed and synthesized as cholesteryl ester transfer protein (CETP) inhibitors. All of them exhibited activity against CETP. Particularly, compounds 24 and 26 displayed the best activity against CETP with the same inhibitory rate of 80.1%.

Inhibitors of the Detoxifying Enzyme of the Phytoalexin Brassinin Based on Quinoline and Isoquinoline Scaffolds

“…Quinolines can be synthesized using a number of classical methods including the Friedländer, Skraup, Combes, and Doebner–von Miller syntheses from anilines and carbonyl compounds, as well as metal-catalyzed dehydrogenative cyclization and other “greener” methods [ 14 , 15 , 16 , 17 ]. In the current work, quinolines 5a – 5f , 6a – 6f and 7a – 7g were synthesized using the Friedländer method by condensation of the corresponding 2-aminobenzaldehydes, prepared from substituted 2-nitrobenzaldehydes [ 18 ], with aldehydes or ketones. In short, 2-nitrobenzaldehydes 11a – 11g were reduced with iron powder to the corresponding amines by refluxing in EtOH/HCl for 40 min [ 19 ].…”

Synthesis and Bioactivity of Quinoline‐3‐carboxamide Derivatives

“…The procedure used by Li et al . for the synthesis of quinoline‐3‐carboxamides was followed with modifications. EDC (0.99 mmol) and 1‐hydroxybenzotrizole (HOBt) (0.99 mmol) were added sequentially at room temperature to the substituted quinoline‐3‐carboxylic acids 4 (0.9 mmol) dissolved in 10 mL DMF.…”

A monofunctional Pt(ii) complex combats triple negative breast cancer by triggering lysosome-dependent cell death

“…Compound 3 was synthesized according to a procedure reported in the literature. 15 L was subsequently synthesized by conjugating compound 2 with 3 using a coupling agent. L was purified and characterized by 1 H, 13 C NMR and ESI-MS (Fig.…”