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
More filters
Journal ArticleDOI
Scope of regioselective Suzuki reactions in the synthesis of arylpyridines and benzylpyridines and subsequent intramolecular cyclizations to azafluorenes and azafluorenones
TL;DR: In this article, the authors investigated regioselective Suzuki reactions of 2,3-dihalopyridines and 2,halo-3-halomethylpyridine bearing synthetic handles for further functionalization.
Journal ArticleDOI
Potential Inhibitors of the Activity of the Cholesterol-Ester Transfer Protein
TL;DR: A group of potential compounds are presented as CETP-inhibitor candidates and the 4F2A_1OB_C_PCW structure was docked with DrugBank-Approved commercial compounds in an extensive database, whose status had already been established from pharmacokinetics and toxicology.
Dissertation
Synthetic Strategies to Access Biologically Important Fluorinated Motifs: Fluoroalkenes and Difluoroketones
Journal ArticleDOI
Highlights on U.S. FDA-approved fluorinated drugs over the past five years (2018-2022).
Saghir Akhtar Ali,Jia Zhou +1 more
TL;DR: A review of fluorine-containing drugs approved by U.S. Food and Drug Administration in the span of past five years (2018-2022) is presented in this article .
References
More filters
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.
Related Papers (5)
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