Design , Synthesis and Biological Evaluation Of Sulfonic Acid Esters / Benzene sulfonamides As Potential CETP Inhibitors

Abstract

Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore it>s a proper target for treating dyslipidemia and related disorders, Guided by our previously-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bio assayed a series of toluene-4-sulfonic acid 4-benzylamino-phcnyl ester (8a-8m)/ N-(4-benzyl-phenyl)-4-methyl- benzene sulfonamide (6a-61) derivatives. The proposed structures for compounds 6a-1 and 8a-m were confirmed via elemental analyses, IR spectroscopy. mass spectroscopy, lH- and 13C-NMR spectra. The most potent synthesized compound 6j illustrated anti-CETP ICSO 0f 3.4 uM.