Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Catherine Sekerke"'
Autor:
Graeme Bainbridge, Nicole Caspers, Andrew Robertson, Jeffrey A. Pfefferkorn, Yuntao Song, Lisa Dillon, Catherine Sekerke, Jeffrey C. Hanselman, Chulho Choi, Gina Lu, Valerie Askew, Zhiwu Lin, Alexander Pavlovsky, Bharat K. Trivedi, Bruce Auerbach, Scott D. Larsen, Melissa S. Harris
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4531-4537
Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models an
Autor:
Jeffrey A. Pfefferkorn, Lisa Dillon, Larry D. Bratton, Bruce Auerbach, Bharat K. Trivedi, Jeffrey C. Hanselman, Scott D. Larsen, Andrew Robertson, Catherine Sekerke, Gina Lu, Paul C. Unangst, Chulho Choi, Karl Olsen
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:5576-5589
In an effort to identify hepatoselective inhibitors of HMG-CoA reductase, two series of pyrroles were synthesized and evaluated. Efforts were made to modify (3R,5R)-7-[3-(4-fluorophenyl)-1-isopropyl-4-phenyl-5-phenylcarbamoyl-1H-pyrrol-2-yl]-3,5-dihy
Autor:
Yuntao Song, Jeffrey C. Hanselman, Xue-Min Cheng, Scott D. Larsen, Zhiwu Lin, Bharat K. Trivedi, Graeme Bainbridge, Alexander Pavlovsky, Larry D. Bratton, Andrew Robertson, Paul C. Unangst, Jeffrey A. Pfefferkorn, Melissa S. Harris, Lisa Dillon, Bruce Auerbach, Erasga Noe Ouano, Chitase Lee, Chulho Choi, Karl Olsen, Catherine Sekerke, Toni Jo Poel, Nicole Caspers, Matthias Eberstadt, Kuai Lin Sun, Steven R. Miller, Roderick Joseph Sorenson, Gina Lu, Valerie Askew, Thomas E. Mertz, Huifen Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4538-4544
This manuscript describes the design and synthesis of a series of pyrrole-based inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia. Analogs were optimized using structure-based design and physical property considerations result
Autor:
Erasga Noe Ouano, David C. Boyles, Chitase Lee, Vaishali Sahasrabudhe, Emi Kimoto, Mark C. Kowala, Yurong Lai, Jonathan Chupka, Bharat K. Trivedi, Xue-Min Cheng, Jeffrey C. Hanselman, Valerie Askew, Zhiwu Lin, P. L. Barclay, Bruce Auerbach, David B. Duignan, Jeffrey A. Pfefferkorn, Theunis C. Goosen, Bo Feng, Lisa Dillon, Richard H. Hutchings, Andrew Robertson, Robert M. Kennedy, Bradley D. Tait, Ayman El-Kattan, Scott D. Larsen, Gina Lu, Daniel Merritt Bowles, Vu Le, Mark Milad, Erick Kindt, Karl Olsen, Mark Richard Bush, John Litchfield, Carine Boustany, Rebecca Bakker-Arkema, Renato J. Scialis, Yi An Bi, Catherine Sekerke, Jaap Mandema, Karen Atkinson
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(9)
The design of drugs with selective tissue distribution can be an effective strategy for enhancing efficacy and safety, but understanding the translation of preclinical tissue distribution data to the clinic remains an important challenge. As part of
Autor:
J. A. Picard, M. K. Shaw, W. H. Roark, R. L. Stanfield, Roger S. Newton, Bruce David Roth, Drago Robert Sliskovic, B.R. Krause, C. J. Blankley, Catherine Sekerke
Publikováno v:
Journal of Medicinal Chemistry. 35:2095-2103
A series of N-heteroaryl-substituted mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and in vivo, and to lower plasma cholesterol in a hypercholesterolemic dog model. The goal of th
Autor:
Richard H. Hutchings, Gina Lu, William Keun Chan Park, Mark C. Kowala, Melissa S. Harris, Chulho Choi, Valerie Askew, Bradley D. Tait, Catherine Sekerke, Scott D. Larsen, Jeffrey A. Pfefferkorn, Lisa Dillon, Alexander Pavlovsky, Nicole Caspers, Graeme Bainbridge, Bruce Auerbach, Jeffrey C. Hanselman, Andrew Robertson, Zhiwu Lin
Publikováno v:
Journal of medicinal chemistry. 51(1)
In light of accumulating evidence that aggressive LDL-lowering therapy may offer increased protection against coronary heart disease, we undertook the design and synthesis of a novel series of HMG-CoA reductase inhibitors based upon a substituted pyr
Autor:
Andrew Robertson, Gina Lu, Catherine Sekerke, Bruce A. Steinbaugh, Robert M. Kennedy, Scott D. Larsen, Bruce D. Roth, Mark C. Kowala, Valerie Askew, Bharat K. Trivedi, Kevin Sun, Steve Miller, Yuntao Song, Jeffrey C. Hanselman, Lisa Dillon, William Keun Chan Park, Bradley D. Tait, Bruce Auerbach, Zhiwu Lin
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(3)
4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3 + 2] cycloaddition of a Munchnone with a sulfonamide-substitut
Autor:
Andrew Robertson, Bruce Auerbach, Scott D. Larsen, Kevin J. Filipski, Toni Jo Poel, Roderick Joseph Sorenson, Jeffrey A. Pfefferkorn, Jeffrey T. Kohrt, Gina Lu, Lisa Dillon, Catherine Sekerke, Jeffrey C. Hanselman, Valerie Askew, Bradley D. Tait, Mark C. Kowala
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(20)
An extraordinarily potent and hepatoselective class of HMG-CoA reductase inhibitors containing a pyrazole core was recently reported; however, its development was hampered by a long and difficult synthetic route. We attempted to circumvent this obsta
Autor:
Naijia Huang, Catherine Sekerke, Y. Y. Shum, Gary A. Walter, Lloyd R. Whitfield, Ann Black, Tsun Chang
Publikováno v:
Therapeutic drug monitoring. 20(1)
An HMG-CoA reductase inhibition assay was developed and validated for quantitation of atorvastatin in human, dog, rat, and mouse plasma. Atorvastatin was isolated from plasma by protein precipitation. Rat-liver microsomes were used to provide the red
Autor:
M. K. Shaw, E. Ferguson, W. H. Roark, J. A. Picard, Bruce David Roth, Catherine Sekerke, Roger S. Newton, Drago Robert Sliskovic, B.R. Krause
Publikováno v:
Journal of medicinal chemistry. 34(1)
A series of substituted quinoline mevalonolactones were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase both in vitro and (cholesterol biosynthesis) in vivo. Since previous studies suggested that the 4-(4-fluorophenyl