Design of a novel class of biphenyl CETP inhibitors

A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound ( 12d) has shown an ability to raise HDL significantly in transgenic mouse PD model. A new class of CETP inhibitors was designed and prepared. These compounds are...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (24), p.7469-7472
Main Authors: Lu, Zhijian, Napolitano, Joann B., Theberge, Ashleigh, Ali, Amjad, Hammond, Milton L., Tan, Eugene, Tong, Xinchun, Xu, Suoyu S., Latham, Melanie J., Peterson, Laurence B., Anderson, Matt S., Eveland, Suzanne S., Guo, Qiu, Hyland, Sheryl A., Milot, Denise P., Chen, Ying, Sparrow, Carl P., Wright, Samuel D., Sinclair, Peter J.
Format: Article
Language:English
Subjects:
Animals
Benzylamines - chemical synthesis
Benzylamines - chemistry
Benzylamines - pharmacology
Biological and medical sciences
Biphenyl
Biphenyl Compounds - chemical synthesis
Biphenyl Compounds - chemistry
Biphenyl Compounds - pharmacology
Carbamates - chemical synthesis
Carbamates - chemistry
Carbamates - pharmacology
Cardiovascular system
CETP inhibitors
Cholesterol Ester Transfer Proteins - antagonists & inhibitors
Cholesterol Ester Transfer Proteins - metabolism
Disease Models, Animal
Drug Design
General and cellular metabolism. Vitamins
HDL-C
Lipoproteins, HDL - metabolism
Medical sciences
Mice
Mice, Transgenic
Miscellaneous
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound ( 12d) has shown an ability to raise HDL significantly in transgenic mouse PD model. A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound ( 12d) has shown an ability to raise HDL significantly in transgenic mouse PD model.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.10.019