Cholesteryl Ester Transfer Protein Inhibitory Activity of New 4-Bromophenethyl Benzamides

نویسندگان

چکیده

Cardiovascular diseases, as coronary heart disease, failure, and hypertension are the first leading cause of death in United States third globally. CETP is a glycoprotein excreted mainly from liver found plasma. Normal plasma concentration 1-4 µg/ml, while ratio increased 70-80% dyslipidemic patients. There growing need for new inhibitors which encourages us to conduct this research. In work, synthesis vitro study four 4-bromophenethylbenzamides 9a-d were carried out. showed that targeted compounds exhibit acceptable activity against CETP, where compound 9a has % inhibition 40.7 at 10 µM concentration. It was presence oxy group both 9c enhances their could be attributed Hydrogen-bond formation with amino acid residues binding site.

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Plasma cholesteryl ester transfer protein.

The plasma lipoproteins are continuously remodeled during their transit through the plasma compartment, owing to the action of lipid metabolizing enzymes and lipid transfer processes. These activities have a major effect on the composition, size, and concentration of the lipoproteins. Lipid transfer processes involving neutral lipids and phospholipids are mediated by specialized plasma proteins...

متن کامل

Plasma concentrations of cholesteryl ester transfer protein in hyperlipoproteinemia. Relation to cholesteryl ester transfer protein activity and other lipoprotein variables.

Cholesteryl ester transfer protein (CETP) mediates an important pathway for reverse cholesterol transport. Concentrations of CETP in fasting plasma were measured by radioimmunoassay in two different groups of hyperlipoproteinemic subjects. Plasma CETP concentrations measured by radioimmunoassay correlated closely with cholesterol ester transfer activity in normal plasma (r = 0.86). In the first...

متن کامل

Immunospecific scintillation proximity assay of cholesteryl ester transfer protein activity.

We describe a novel, immunospecific scintillation proximity assay for determining cholesteryl ester transfer protein (CETP) activity in total human serum and in reconstituted experimental mixtures. The assay is based on the measurement of radiolabeled cholesteryl esters transferred from a tracer dose of biosynthetically labeled high-density lipoprotein subfraction 3 to unlabeled apolipoprotein ...

متن کامل

Accelerated Cholesteryl Ester Transfer

To discern the mechanism(s) that underlie abnormal cholesteryl ester transfer (CET) in patients with hypercholesterolemia, we have studied this dysfunctional step in reverse cholesterol transport in 13 subjects with genetically heterogeneous forms of hypercholesterolemia (HC). In all HC patients, the mass of CE transferred in whole plasma from HDL to VLDL and LDL increased rapidly initially and...

متن کامل

Transfer of cholesteryl ester into high density lipoprotein by cholesteryl ester transfer protein: effect of HDL lipid and apoprotein content.

Recombinant high density lipoprotein (rHDL) particles were prepared by cosonication of purified lipids and human apoproteins and incubated with partly purified cholesteryl ester transfer protein (CETP) and low density lipoprotein (LDL) containing [3H]cholesteryl ester. Increasing the triglyceride content relative to cholesteryl ester in rHDL significantly decreased the ability of the particles ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Jordan Journal of Pharmaceutical Sciences

سال: 2023

ISSN: ['1995-7157', '2707-6253']

DOI: https://doi.org/10.35516/jjps.v16i2.1465