Design, synthesis, and biological evaluation of benzylamino-methanone based cholesteryl ester transfer protein inhibitors.
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 its a proper target 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 benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 microM.
Abu Sheikha
Ghassan
G
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Zaytoonah Private University of Jordan, Amman, Jordan.
Abu Khalaf
Reema
R
Melhem
Areej
A
Albadawi
Ghadeer
G
D000818:Animals; D048588:Benzoxazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001593:Benzyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D021281:Quantitative Structure-Activity Relationship; D011817:Rabbits
D048588:Benzoxazines; D001593:Benzyl Compounds; D053480:Cholesterol Ester Transfer Proteins