Výsledky vyhledávání - "Gary B. Phillips"

GS-5759, a Bifunctional β2-Adrenoceptor Agonist and Phosphodiesterase 4 Inhibitor for Chronic Obstructive Pulmonary Disease with a Unique Mode of Action: Effects on Gene Expression in Human Airway Epithelial Cells

Autor: Musong Kim, Mark A. Giembycz, Taruna Joshi, Dong Yan, Robert Newton, Omar Hamed, Gary B. Phillips, Michael Salmon, Clifford D. Wright, Stacey L. Tannheimer

Publikováno v: The Journal of pharmacology and experimental therapeutics. 360(2)

(R)-6-[(3-{[4-(5-{[2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}pent-1-yn-1-yl)phenyl] carbamoyl}phenyl)sulphonyl]-4-[(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide trifluoroacetic acid (GS-5759) is a bifunctional ligand

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ec5a2ff92e40be17acdbca537369144
https://pubmed.ncbi.nlm.nih.gov/27927912

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The in vitro pharmacology of GS-5759, a novel bifunctional phosphodiesterase 4 inhibitor and long acting β2-adrenoceptor agonist

Autor: Michael Salmon, Leena Patel, Stacey L. Tannheimer, Clifford D. Wright, Musong Kim, Gary B. Phillips, Zhi Hua Cui, William R. Baker, Eric A. Sorensen

Publikováno v: The Journal of pharmacology and experimental therapeutics. 349(1)

Inhaled long-acting β(2)-adrenoceptor agonists (LABA) that act as bronchodilators and the oral anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor roflumilast are both approved therapies for chronic obstructive pulmonary disease (COPD). Here we d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ec1f00994e36decfd1eb9ed38147c53
https://pubmed.ncbi.nlm.nih.gov/24513870

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Solid phase synthesis of benzimidazolones

Autor: Guo Ping Wei, Gary B. Phillips

Publikováno v: Tetrahedron Letters. 39:179-182

An efficient solid phase synthesis of benzimidazol-2-one-5 carboxylic acid is described. Polymer bound o-fluoronitroaromatic compound 2 was treated with an amine to give o-nitroaniline derivative 3 . Reduction of 3 with SnCl 2 followed by cyclization

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ae7db38096f3565094d181a995045136
https://doi.org/10.1016/s0040-4039(97)10518-4

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Design, synthesis, and biological activity of novel factor Xa inhibitors: 4-aryloxy substituents of 2,6-diphenoxypyridines

Publikováno v: Bioorganicmedicinal chemistry. 10(3)

A novel series of triaryloxypyridines have been designed to inhibit factor Xa, a serine protease strategically located in the coagulation cascade. Inhibitor 5e has a K(I) against factor Xa of 0.12nM and is greater than 8000- and 2000-fold selective o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::1bd13ce372a62c76678fbca6b4b17c2f
https://pubmed.ncbi.nlm.nih.gov/11814853

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Mechanistic studies with potent and selective inducible nitric-oxide synthase dimerization inhibitors

Autor: Douglas S. Auld, Marc Whitlow, Charles B. Glaser, Kirk McMillan, Mark A. Polokoff, Wei Xia, James J. Devlin, Gary B. Phillips, Richard I. Feldman, Dennis J. Stuehr, Sanjay Ghosh, Eric Blasko, John Parkinson

Publikováno v: The Journal of biological chemistry. 277(1)

A series of potent and selective inducible nitric-oxide synthase (iNOS) inhibitors was shown to prevent iNOS dimerization in cells and inhibit iNOS in vivo. These inhibitors are now shown to block dimerization of purified human iNOS monomers. A 3H-la

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca01ed3b92db5b3392fa793cffad6a08
https://pubmed.ncbi.nlm.nih.gov/11689556

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Synthesis, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents

Autor: Mark E. Sullivan, Thomas M. Argentieri, Robert P. Gomez, Thomas Kenneth Morgan, Gary B. Phillips, William C. Lumma, Joan M. Lind, Randall Lis

Publikováno v: Journal of medicinal chemistry. 35(4)

A series of novel arylpiperazines have been prepared in an attempt to incorporate both class II (beta-receptor blocking) and class III antiarrhythmic properties in a single molecule. The key step in the preparation of the new compounds involves a reg

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d1ae941855d9670f1d865112f182d8d
https://pubmed.ncbi.nlm.nih.gov/1347318

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Synthesis and cardiac electrophysiological activity of aryl-substituted derivatives of the class III antiarrhythmic agent sematilide. Potential class I/III agents

Autor: Klaus Nickisch, Mark E. Sullivan, Thomas M. Argentieri, Thomas Kenneth Morgan, Gary B. Phillips, Ronald A. Wohl, Robert P. Gomez, Joan M. Lind

Publikováno v: Journal of medicinal chemistry. 33(2)

Twelve novel derivatives of the selective class III antiarrhythmic agent sematilide were prepared in an attempt to incorporate both class I and class III electrophysiological properties into a single molecule. Electrophysiological activity was determ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a48a8a2303bf7fdaaa833b81a8c6959d
https://pubmed.ncbi.nlm.nih.gov/2299628

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