Design, synthesis, and biological evaluation of sulfonic acid ester and benzenesulfonamide derivatives as potential CETP inhibitors was written by Abu Khalaf, Reema;Abu Sheikha, Ghassan;Al-Sha’er, Mahmoud;Albadawi, Ghadeer;Taha, Mutasem. And the article was included in Medicinal Chemistry Research in 2012.Category: amides-buliding-blocks This article mentions the following:
Epidemiol. studies have established an inverse relationship between plasma high-d. lipoprotein (HDL) cholesterol concentration, and incidence of coronary artery disease (CAD); thus, the development of novel therapies that attempt to exploit the atheroprotective functions of HDL is a major goal. Inhibition of cholesteryl ester transfer protein (CETP) is one of the approaches targeted to increase HDL cholesterol concentration CETP is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between HDL and low-d. lipoproteins (LDL), and therefore CETP inhibitors could be useful agents in the future for treating dyslipidemia and related disorders. Guided by our previously reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of sulfonic acid ester and benzenesulfonamide derivatives that can serve as a promising lead compounds for the development of potential and selective CETP inhibitors. The most potent compound 6k illustrated an IC50 of 3.4 μM. In the experiment, the researchers used many compounds, for example, N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6Category: amides-buliding-blocks).
N-(4-Hydroxyphenyl)-4-methylbenzenesulfonamide (cas: 1146-43-6) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics