Journal ArticleDOI
Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors.
Michael M. Miller,Yalei Liu,Ji Jiang,James A. Johnson,Muthoni G. Kamau,David S. Nirschl,Yufeng Wang,Lalgudi S. Harikrishnan,David S. Taylor,Alice Ye A. Chen,Xiaohong Yin,Ramakrishna Seethala,Tara L. Peterson,Tatyana Zvyaga,Jun Zhang,Christine Huang,Ruth R. Wexler,Michael A. Poss,R. Michael Lawrence,Leonard P. Adam,Mark E. Salvati +20 more
TLDR
A novel series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein is described, and optimization of the urea moiety is explored to balance in vitro metabolic stability with CETP potency in the whole plasma assay.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2012-10-15. It has received 19 citations till now. The article focuses on the topics: Cholesterylester transfer protein & Sterol O-acyltransferase.read more
Citations
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Journal ArticleDOI
2D and 3D QSAR models for identifying diphenylpyridylethanamine based inhibitors against cholesteryl ester transfer protein.
TL;DR: 2D and 3D QSAR models-based a series of diphenylpyridylethanamine derivatives (DPPE) derivatives were performed to elucidate structural and physicochemical requirements for higher CETP inhibitory activity and twelve newly designed DPPE derivatives were proposed to be robust and potent CETP inhibitors.
Journal ArticleDOI
Microwave-assisted transamidation of ureas
Tammy C. Wang,Jennifer X. Qiao +1 more
TL;DR: In this paper, an effective microwave assisted urea formation from cyclopentyl- or isopropyl-substituted ureas is described using microwave irradiation.
Journal ArticleDOI
Expeditious novel routes to enantiopure 3-amino tetrahydrofuran hydrochloride
TL;DR: In this article, the synthesis of chemically and enantiomerically pure (S)-3-amino tetrahydrofuran hydrochloride starting from the natural amino acids, l -aspartic acid or l -methionine is described.
Journal ArticleDOI
Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors
Yufeng Wang,Wu Yang,Heather Finlay,Lalgudi S. Harikrishnan,Ji Jiang,Muthoni G. Kamau,Katy Van Kirk,David S. Nirschl,David S. Taylor,Alice Ye A. Chen,Xiaohong Yin,Paul G. Sleph,Richard Yang,Christine Huang,Leonard P. Adam,R. Michael Lawrence,Ruth R. Wexler,Mark E. Salvati +17 more
TL;DR: A series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein with aminoheterocycles appended onto the N-terminus of the chemotype were explored as urea mimetics to improve metabolic stability and PXR transactivation profile.
Journal ArticleDOI
Phenanthroimidazole derivatives act as potentinducer of autophagy by activating DNA damage pathway.
TL;DR: Multiple effects, especially induction apoptosis and autophagy, indicate the potential of 6 for development as a novel anticancer drug.
References
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Journal ArticleDOI
Prevention of coronary heart disease with pravastatin in men with hypercholesterolemia. West of Scotland Coronary Prevention Study Group
J. Shepherd,Stuart M. Cobbe,Ian Ford,C. G. Isles,AR Lorimer,Peter W. Macfarlane,J. H. Mckillop,Christopher J. Packard +7 more
TL;DR: Treatment with pravastatin significantly reduced the incidence of myocardial infarction and death from cardiovascular causes without adversely affecting the risk of death from noncardiovascular causes in men with moderate hypercholesterolemia and no history of my Cardiac Infarction.
Journal Article
MRC/BHF Heart Protection Study of cholesterol lowering with simvastatin in 20536 high-risk individuals: a randomised placebo-controlled trial. Commentary
TL;DR: Adding simvastatin to existing treatments safely produces substantial additional benefits for a wide range of high-risk patients, irrespective of their initial cholesterol concentrations.
Journal ArticleDOI
Primary Prevention of Acute Coronary Events With Lovastatin in Men and Women With Average Cholesterol Levels: Results of AFCAPS/TexCAPS
John R. Downs,Michael Clearfield,Stephen E. Weis,Edwin J. Whitney,Deborah R. Shapiro,Polly A. Beere,Alexandra Langendorfer,Evan A. Stein,William Kruyer,Antonio M. Gotto +9 more
TL;DR: Lovastatin reduces the risk for the first acute major coronary event in men and women with average TC and LDL-C levels and below-average HDL- C levels and supports the inclusion of HDL-C in risk-factor assessment and the need for reassessment of the National Cholesterol Program guidelines.
Journal ArticleDOI
High density lipoprotein as a protective factor against coronary heart disease: The Framingham study
TL;DR: The major potent lipid risk factor was HDL cholesterol, which had an inverse association with the incidence of coronary heart disease in either men or women and these associations were equally significant even when other lipids and other standard risk factors for coronaryHeart disease were taken into consideration.
Journal ArticleDOI
Prevention of coronary and stroke events with atorvastatin in hypertensive patients who have average or lower-than-average cholesterol concentrations, in the Anglo-Scandinavian Cardiac Outcomes Trial—Lipid Lowering Arm (ASCOT-LLA): a multicentre randomised controlled trial
Peter S. Sever,Björn Dahlöf,Neil R Poulter,Hans Wedel,Gareth Beevers,Mark J. Caulfield,Rory Collins,Sverre E. Kjeldsen,Arni Kristinsson,Gordon T. McInnes,Jesper Mehlsen,Markku S. Nieminen,Eoin O'Brien,Jan Östergren +13 more
TL;DR: The reductions in major cardiovascular events with atorvastatin are large, given the short follow-up time, and may have implications for future lipid-lowering guidelines.
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Inhibition of Cholesteryl Ester Transfer Protein Preserves High-Density Lipoprotein Cholesterol and Improves Survival in Sepsis.
Mark Trinder,Yanan Wang,Christian M. Madsen,Christian M. Madsen,Tatjana Ponomarev,Lubos Bohunek,Brendan A. Daisely,HyeJin Julia Kong,Lisanne L. Blauw,Børge G. Nordestgaard,Anne Tybjærg-Hansen,Mark M. Wurfel,James A. Russell,James A. Russell,Keith R. Walley,Keith R. Walley,Patrick C.N. Rensen,John H. Boyd,Liam R. Brunham +18 more