Ezetimibe analogs with a reorganized azetidinone ring: Design, synthesis, and evaluation of cholesterol absorption inhibitions

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 1, 2007, Pages 101-104

  Xu, Xianxiu ^a,b   Fu, Renzhong ^a   Chen, Jin ^a   Chen, Shengwu ^c   Bai, Xu ^a,b  

^a JILIN UNIVERSITY   (China)

^b Changchun Discovery Sciences Ltd   (China)

^c Jilin Natural Pharmatech Co Ltd   (China)

Author keywords

Azetidin 2 one; Backbone re organized ezetimibe analogs; Cholesterol absorption inhibition

Indexed keywords

AZETIDINONE DERIVATIVE; CHOLESTEROL; EZETIMIBE; EZETIMIBE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL DIET; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; LIPID ABSORPTION; LIPID DIET; NONHUMAN; PROBABILITY; RAT;

ABSORPTION; ANIMALS; ANTICHOLESTEREMIC AGENTS; AZETIDINES; CHOLESTEROL, DIETARY; CRYSTALLOGRAPHY, X-RAY; DIET, ATHEROGENIC; DRUG DESIGN; MOLECULAR STRUCTURE; RATS; STEREOISOMERISM;

RATTUS;

EID: 33845600703     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.09.078     Document Type: Article

References (26)

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26. Cholesterol-feeding experiment: Male Wistar rats with weight of 150-180 g were purchased from the Center of Research Animals, the College of Basic Medicines, Jilin University. The high-fat and high-cholesterol diet was made from 87.8% regular feeds, 2% cholesterol, 10% hog fat, and 0.2% propylthiouracil. The animals were raised for 1 week, divided into individual groups according to their levels of TC and LDL-cholesterol in serum, and then fed for 2 weeks on regular diet, high-fat and high-cholesterol diet, high-fat and high-cholesterol diet with ezetimibe or individual drugs, respectively. The drugs were made to a mixture with 0.5% sodium carboxy methyl cellulose(40 mg/100 ml), administered at a single dosage of 4 mg/kg/day by intragastric perfusion. After fasted for 16 h, blood samples were collected by cutting the tails, and the serum was isolated and measured for the level of total cholesterol and LDL-cholesterol. The data were calculated by statistical methods.