Original articlePharmacophore-based design, synthesis, and biological evaluation of novel 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides as cholesteryl ester transfer protein (CETP) inhibitors

Add time:08/21/2019    Source:sciencedirect.com

Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol (LDL-C) levels. Inhibition of CETP may be a new therapy for treating atherosclerosis. Herein, we report the development of a ligand-based pharmacophore model and pharmacophore-based virtual screening of the ZINC/big-n-greasy database, leading to the identification of compound H-10 as a potential CETP inhibitor in vitro. Based on H-10, a series of 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides were designed, synthesized, and evaluated against CETP. Compound 4l was found to have the best activity, resulting in 85.0% inhibition of CETP at 10 μmol/L.

We also recommend Trading Suppliers and Manufacturers of 3-(3,4-dichlorophenyl)-2-Propynoic acid (cas 19498-74-9). Pls Click Website Link as below: cas 19498-74-9 suppliers

Prev:Synthesis and antimicrobial activity of 3-(2-thienyl)-4-arylazo-5-hydroxy-5-trifluoromethyl-Δ2-isoxazolines and 3-(2-thienyl)-4-arylazo-5-trifluoromethylisoxazoles
Next:Selective C–N bond oxidation: demethylation of N-methyl group in N-arylmethyl-N-methyl-α-amino esters utilizing N-iodosuccinimide (NIS))