Search Results - "Doherty, James B."

Synthesis and biological activity of pyridopyridazin-6-one p38 MAP kinase inhibitors. Part 1 by Tynebor, Robert M., Chen, Meng-Hsin, Natarajan, Swaminathan R., O’Neill, Edward A., Thompson, James E., Fitzgerald, Catherine E., O’Keefe, Stephen J., Doherty, James B.

“…The development and synthesis of potent p38α MAP kinase inhibitors containing a pyridazinone platform is described. Evolution of the p38α selective…”
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Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase by Stelmach, John E., Liu, Luping, Patel, Sangita B., Pivnichny, James V., Scapin, Giovanna, Singh, Suresh, Hop, Cornelis E.C.A., Wang, Zhen, Strauss, John R., Cameron, Patricia M., Nichols, Elizabeth A., O'Keefe, Stephen J., O'Neill, Edward A., Schmatz, Dennis M., Schwartz, Cheryl D., Thompson, Chris M., Zaller, Dennis M., Doherty, James B.

“…The development of potent, orally bioavailable (in rat) and selective dihydroquinazolinone inhibitors of p38α MAP kinase is described. These analogues are…”
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Selective, direct activation of high-conductance, calcium-activated potassium channels causes smooth muscle relaxation by Ponte, Cristiano G, McManus, Owen B, Schmalhofer, William A, Shen, Dong-Ming, Dai, Ge, Stevenson, Andra, Sur, Sylvie, Shah, Tarak, Kiss, Laszlo, Shu, Min, Doherty, James B, Nargund, Ravi, Kaczorowski, Gregory J, Suarez-Kurtz, Guilherme, Garcia, Maria L

“…High-conductance calcium-activated potassium (Maxi-K) channels are present in smooth muscle where they regulate tone. Activation of Maxi-K channels causes…”
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Synthesis and biological activity of pyridopyridazin-6-one p38α MAP kinase inhibitors. Part 2 by Tynebor, Robert M., Chen, Meng-Hsin, Natarajan, Swaminathan R., O’Neill, Edward A., Thompson, James E., Fitzgerald, Catherine E., O’Keefe, Stephen J., Doherty, James B.

“…This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38α activity and…”
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Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors by Chen, Meng-Hsin, Fitzgerald, Patricia, Singh, Suresh B., O’Neill, Edward A., Schwartz, Cheryl D., Thompson, Chris M., O’Keefe, Stephen J., Zaller, Dennis M., Doherty, James B.

“…The synthesis and biological activities of some quinolinone and dihydroquinolinone p38 MAP kinase inhibitors are reported. Modifications to the…”
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P38 MAP kinase inhibitors: evolution of imidazole-based and pyrido-pyrimidin-2-one lead classes by Natarajan, Swaminathan R, Doherty, James B

“…The initial disclosure of tri-substituted imidazole-based drug molecules such as 1 for inhibition of p38 MAP kinase by SmithKline Beecham (SB) sparked an…”
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Synthesis and biological activity of 2H-quinolizin-2-one based p38α MAP kinase inhibitors by TYNEBOR, Robert M, CHEN, Meng-Hsin, NATARAJAN, Swaminathan R, O'NEILL, Edward A, THOMPSON, James E, FITZGERALD, Catherine E, O'KEEFE, Stephen J, DOHERTY, James B

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SAR of 3,4-Dihydropyrido[3,2- d]pyrimidone p38 inhibitors by Liu, Luping, Stelmach, John E., Natarajan, Swaminathan R., Chen, Meng-Hsin, Singh, Suresh B., Schwartz, Cheryl D., Fitzgerald, Catherine E., O'Keefe, Stephen J., Zaller, Dennis M., Schmatz, Dennis M., Doherty, James B.

“…Development for a class of potent 3,4-dihydropyrido(3,2- d)pyrimidone inhibitors of p38a MAP kinase is described. Modification of N-1 aryl and C-6 arylsulfide…”
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Hybrid-Designed Inhibitors of p38 MAP Kinase Utilizing N-Arylpyridazinones by Colletti, Steven L, Frie, Jessica L, Dixon, Elizabeth C, Singh, Suresh B, Choi, Bernard K, Scapin, Giovanna, Fitzgerald, Catherine E, Kumar, Sanjeev, Nichols, Elizabeth A, O'Keefe, Stephen J, O'Neill, Edward A, Porter, Gene, Samuel, Koppara, Schmatz, Dennis M, Schwartz, Cheryl D, Shoop, Wesley L, Thompson, Chris M, Thompson, James E, Wang, Ruixiu, Woods, Andrea, Zaller, Dennis M, Doherty, James B

“…Imidazo[1,2-a]pyridyl N-arylpyridazinones were hybridized from the classic pyridinylimidazoles and the more recent dual hydrogen bond acceptors, resulting in a…”
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p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones by Hunt, Julianne A, Kallashi, Florida, Ruzek, Rowena D, Sinclair, Peter J, Ita, Ida, McCormick, Sherrie X, Pivnichny, James V, Hop, C.E.C.A, Kumar, Sanjeev, Wang, Zhen, O'Keefe, Stephen J, O'Neill, Edward A, Porter, Gene, Thompson, James E, Woods, Andrea, Zaller, Dennis M, Doherty, James B

“…We have synthesized a series of C7-piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones that are highly…”
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p38 MAP kinase inhibitors: Metabolically stabilized piperidine-substituted quinolinones and naphthyridinones by Bao, Jianming, Hunt, Julianne A., Miao, Shouwu, Rupprecht, Kathleen M., Stelmach, John E., Liu, Luping, Ruzek, Rowena D., Sinclair, Peter J., Pivnichny, James V., Hop, Cornelis E.C.A., Kumar, Sanjeev, Zaller, Dennis M., Shoop, Wesley L., O’Neill, Edward A., O’Keefe, Stephen J., Thompson, Chris M., Cubbon, Rose M., Wang, Ruixiu, Zhang, Wen Xiao, Thompson, James E., Doherty, James B.

“…Quinolinones and naphthyridinones with C7 N- t-butyl piperidine substituents were found to be potent p38 MAP kinase inhibitors. These compounds significantly…”
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p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold by Natarajan, Swaminathan R, Wisnoski, David D, Singh, Suresh B, Stelmach, John E, O'Neill, Edward A, Schwartz, Cheryl D, Thompson, Chris M, Fitzgerald, Catherine E, O'Keefe, Stephen J, Kumar, Sanjeev, Hop, Cornelis E C A, Zaller, Dennis M, Schmatz, Dennis M, Doherty, James B

“…A new class of p38 antagonists based on 3,4-dihydropyrido[3,2,-d]pyrimidine scaffold has been developed. These inhibitors exhibit unprecedented selectivity…”
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Cephalosporin antibiotics can be modified to inhibit human leukocyte elastase by Doherty, James B, Ashe, Bonnie M, Argenbright, Lawrence W, Barker, Peter L, Bonney, Robert J, Chandler, Gilbert O, Dahlgren, Mary Ellen, Dorn, Conrad P, Finke, Paul E, Firestone, Raymond A, Fletcher, Daniel, Hagmann, William K, Mumford, Richard, O'Grady, Laura, Maycock, Alan L, Pisano, Judith M, Shah, Shrenik K, Thompson, Kevan R, Zimmerman, Morris

“…Several laboratories, including our own have reported the synthesis and activity of certain low relative molecular mass inhibitors of mammalian serine…”
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Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters by Doherty, James B, Ashe, Bonnie M, Barker, Peter L, Blacklock, Thomas J, Butcher, John W, Chandler, Gilbert O, Dahlgren, M. Ellen, Davies, Philip, Dorn, Conrad P

“…Time-dependent inhibitors of the enzyme human leukocyte elastase have been developed based on the cephem nucleus. A series of cephalosporin tert-butyl esters…”
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Crystallographie study of a β -lactam inhibitor complex with elastase at 1.84 Å resolution by Navia, Manuel A, Springer, James P, Lin, Tsau-Yen, Williams, Hollis R, Firestone, Raymond A, Pisano, Judith M, Doherty, James B, Finke, Paul E, Hoogsteen, Karst

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Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins by Shah, Shrenik K, Brause, Karen A, Chandler, Gilbert O, Finke, Paul E, Ashe, Bonnie M, Weston, Hazel, Knight, Wilson B, Maycock, Alan L, Doherty, James B

“…Several 3'-substituted cephalosporin sulfones were synthesized from 3-(hydroxymethyl)cephalosporin, which was prepared by Ti(OiPr)4 hydrolysis of the…”
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Synthesis and biological activity of pyridopyridazin-6-one p38[alpha] MAP kinase inhibitors. Part 2 by Tynebor, Robert M, Chen, Meng-Hsin, Natarajan, Swaminathan R, O'Neill, Edward A, Thompson, James E, Fitzgerald, Catherine E, O'Keefe, Stephen J, Doherty, James B

“…This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38[alpha]…”
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beta.-Cyclodextrinylbisimidazole, a model for ribonuclease by Breslow, Ronald, Doherty, James B, Guillot, Genevieve, Lipsey, Carol

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Synthesis and biological activity of 2H-quinolizin-2-one based p38a MAP kinase inhibitors by Tynebor, Robert M, Chen, Meng-Hsin, Natarajan, Swaminathan R, O'Neill, Edward A, Thompson, James E, Fitzgerald, Catherine E, O'Keefe, Stephen J, Doherty, James B

“…The development and synthesis of potent p38a MAP kinase inhibitors containing a 2H-quinolizin-2-one platform is described. Evolution of the 2H-quinolizin-2-one…”
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Synthesis and biological activity of 2 H-quinolizin-2-one based p38α MAP kinase inhibitors by Tynebor, Robert M., Chen, Meng-Hsin, Natarajan, Swaminathan R., O’Neill, Edward A., Thompson, James E., Fitzgerald, Catherine E., O’Keefe, Stephen J., Doherty, James B.

“…The development and synthesis of potent p38α MAP kinase inhibitors containing a 2 H-quinolizin-2-one platform is described. Evolution of the 2…”
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