title: Design, synthesis, and biological evaluation of benzylamino-methanone based cholesteryl ester transfer protein 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 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.
authors: Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Zaytoonah Private University of Jordan, Amman, Jordan.
authors: Ghassan
authors: G
authors: Abu Sheikha
authors: Reema
authors: R
authors: Abu Khalaf
authors: Areej
authors: A
authors: Melhem
authors: Ghadeer
authors: G
authors: Albadawi
mesh_terms: 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
chemical_list: D048588:Benzoxazines; D001593:Benzyl Compounds; D053480:Cholesterol Ester Transfer Proteins