Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Brian R. Bond"'
Autor:
Ying Yu, Brian R. Bond, Jonathan Oliva, Georg Neckermann, Deena Tajfirouz, Marvin J. Meyers, Mary Campbell, Michael J. Prinsen, Stacy D. Arnett, Robert K. M. Choy, Peter G. Ruminski, Yuhua Ji, Eugenio L. de Hostos, David W. Griggs
Publikováno v:
The Journal of Pharmacology and Experimental Therapeutics
Racecadotril (acetorphan) is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals and humans; however, in humans, it suffers from shortcomings that might be improved with newer drugs in this class that have progressed
Autor:
Brian R. Bond, D. Joseph Rogier, Yi Zheng, Maddux Todd Michael, Sharon Lu, Alan MacInnes, Jeanne M. Rumsey, John K. Walker, E. Jon Jacobsen, Robert Hughes, Seungil Han
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6348-6352
We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles.
Autor:
Robert Hughes, Michael B. Tollefson, Michael John Palmer, Brad A. Acker, Brian R. Bond, Fox David Nathan Abraham, Ying Yu, E. J. Jacobsen, John K. Walker, Sandra K. Freeman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3120-3124
1H-Pyrazolo[4,3-d]pyrimidines are a class of potent and selective second generation phosphodiesterase 5 (PDE5) inhibitors. This work explores the potency, selectivity and efficacy of 1-(2-ethoxyethyl)-1H-pyrazolo[4,5-d]pyrimidines as PDE5 inhibitors
Autor:
Brian R. Bond, Michael John Palmer, John K. Walker, Ying Yu, Michael B. Tollefson, Brad A. Acker, Fox David Nathan Abraham, Sandra K. Freeman, Eric Jon Jacobsen, Robert Hughes
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3125-3128
1H-Pyrazolo[4,3-d]pyrimidines were previously disclosed as a potent second generation class of phosphodiesterase 5 (PDE5) inhibitors. This work explores the advancement of more selective and potent PDE5 inhibitors resulting from the substitution of 2
Autor:
Sandra W. Curtiss, D. Joseph Rogier, Alan MacInnes, Brown David L, Mike B. Tollefson, Brian R. Bond, Yvette M. Fobian, Maddux Todd Michael, Dafydd R. Owen, Jeanne M. Rumsey, Brent V. Mischke, Jerry W. Cubbage, Alan G. Benson, Robert Hughes, Lena L Zhang, E. Jon Jacobsen, Steven E. Heasley, Joseph B. Moon, Ying Yu, John M. Molyneaux, Yi Zheng, Brad A. Acker, Blevis-Bal Radhika M, John N. Freskos, John K. Walker, Jennie L. Walgren
Publikováno v:
Journal of Medicinal Chemistry. 53:2656-2660
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[
Autor:
Maddux Todd Michael, Yvette M. Fobian, Alan G. Benson, Dafydd R. Owen, Brian R. Bond, Christopher Phillips, Brad A. Acker, E. Jon Jacobsen, Michael John Palmer, D. Joseph Rogier, John M. Molyneaux, Brent V. Mischke, John N. Freskos, Tracy J. Ringer, Andrew Simon Bell, Blevis-Bal Radhika M, Robert Hughes, David G. Brown, Steve E. Heasley, Joseph B. Moon, John K. Walker, Brown David L, William C. Stallings, Michael B. Tollefson, Alan MacInnes, Jerry W. Cubbage, Yung Yu, Margarita Rodriquez-Lens, Fox David Nathan Abraham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4088-4091
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which s
Autor:
Ying Yu, Haodan Yuan, Jonathan Chupka, Bo Feng, Jenny Y. Zheng, Brian R. Bond, Timothy G. Heath
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 330:191-197
In humans and rats, a synergistic blood pressure reduction was observed when the fibrate gemcabene (CI-1027) was coadministered with the angiotensin-converting enzyme inhibitor quinapril. In a quinapril (3 mg/kg) pharmacokinetic rat study, there was
Autor:
A. Jackson Crumbley, Francis G. Spinale, John M. Kratz, Marlina M. Multani, Scott Reeves, Brian R. Bond, C.Allyson Walker, Scott Walton, B.Hugh Dorman, Mark L. Pinosky, Mark J. Clair, James L. Zellner
Publikováno v:
The Journal of Thoracic and Cardiovascular Surgery. 122:358-364
Objective: Our objectives are 2-fold: (1) to serially measure the release of endothelin and graft-conduit endothelin sensitivity during and after coronary artery bypass grafting and (2) to define potential relationships of changes in endothelin level
Autor:
James H. McElmurray, Y. V. Mukhin, Francis G. Spinale, R.Brent New, Rupak Mukherjee, Brian R. Bond, B.Hugh Dorman
Publikováno v:
Anesthesia & Analgesia. 90:1080-1085
Transient left ventricular (LV) dysfunction can occur after cardioplegic arrest. The contributory mechanisms for this phenomenon are not completely understood. We tested the hypothesis that exposure of LV myocytes to endothelin (ET) during simulated
Publikováno v:
Cardiovascular Research. 46:225-238
A fundamental structural event in the progression of heart failure due to dilated cardiomyopathy is left ventricular (LV) myocardial remodeling. The matrix metalloproteinases (MMPs) are an endogenous family of enzymes which contribute to matrix remod