Search Results - "Brown, Brian S."

Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening by Kumar, Anuradha, Chettiar, Somsundaram, Brown, Brian S., Early, Julie, Ollinger, Juliane, Files, Megan, Bailey, Mai A., Korkegian, Aaron, Dennison, Devon, McNeil, Matthew, Metz, James, Osuma, Augustine, Curtin, Michael, Kunzer, Aaron, Freiberg, Gail, Bruncko, Milan, Kempf, Dale, Parish, Tanya

“…We performed a high-throughput phenotypic whole cell screen of Mycobacterium tuberculosis against a diverse chemical library of approximately 100,000 compounds…”
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Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity by von Geldern, Thomas W, Morton, Howard E, Clark, Rick F, Brown, Brian S, Johnston, Kelly L, Ford, Louise, Specht, Sabine, Carr, Robert A, Stolarik, Deanne F, Ma, Junli, Rieser, Matthew J, Struever, Dominique, Frohberger, Stefan J, Koschel, Marianne, Ehrens, Alexandra, Turner, Joseph D, Hübner, Marc P, Hoerauf, Achim, Taylor, Mark J, Ward, Stephen A, Marsh, Kennan, Kempf, Dale J

“…There is a significant need for improved treatments for onchocerciasis and lymphatic filariasis, diseases caused by filarial worm infection. In particular, an…”
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TRPV1 antagonist, A-889425, inhibits mechanotransmission in a subclass of rat primary afferent neurons following peripheral inflammation by Brederson, Jill-Desiree, Chu, Katharine L., Reilly, Regina M., Brown, Brian S., Kym, Philip R., Jarvis, Michael F., McGaraughty, Steve

“…TRPV1 (transient receptor potential vanilloid family type 1) is a nonselective cation channel that is activated and/or sensitized by noxious heat, protons, and…”
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Antagonism of TRPV1 receptors indirectly modulates activity of thermoregulatory neurons in the medial preoptic area of rats by McGaraughty, Steve, Segreti, Jason A, Fryer, Ryan M, Brown, Brian S, Faltynek, Connie R, Kym, Philip R

“…Abstract In order to enhance understanding of TRPV1 contributions to thermoregulation, we measured the effects of a TRPV1 receptor antagonist, A-889425, on…”
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Asymmetric Synthesis of Oxygen Heterocycles via Pd-Catalyzed Dynamic Kinetic Asymmetric Transformations: Application to Nucleosides by Trost, Barry M., Brown, Brian S., McEachern, Ernest J., Kuhn, Oliver

“…Racemic butadiene and isoprene monoepoxide react with unsaturated alcohols in the presence of a chiral palladium catalyst and a boron co‐catalyst to give…”
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Targeting IRAK3 for Degradation to Enhance IL-12 Pro-inflammatory Cytokine Production by Rowley, Ann, Brown, Brian S., Stofega, Mary, Hoh, Hana, Mathew, Rebecca, Marin, Violeta, Ding, Rong-Xian, McClure, Ryan A., Bittencourt, Fabiola M., Chen, Jun, Gururaja, Tarikere, Kinoshita, Taisei, Wang, Xueqing, Rivkin, Alexey, Woller, Kevin R.

“…Interleukin-1 receptor-associated kinase 3 (IRAK3) is a pseudokinase mediator in the human inflammatory pathway, and ablation of its function is associated…”
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Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design by Hobson, Adrian D, Judge, Russell A, Aguirre, Ana L, Brown, Brian S, Cui, Yifang, Ding, Ping, Dominguez, Eric, DiGiammarino, Enrico, Egan, David A, Freiberg, Gail M, Gopalakrishnan, Sujatha M, Harris, Christopher M, Honore, Marie P, Kage, Karen L, Kapecki, Nicolas J, Ling, Christopher, Ma, Junli, Mack, Helmut, Mamo, Mulugeta, Maurus, Stefan, McRae, Bradford, Moore, Nigel S, Mueller, Bernhard K, Mueller, Reinhold, Namovic, Marian T, Patel, Kaushal, Pratt, Steve D, Putman, C. Brent, Queeney, Kara L, Sarris, Kathy K, Schaffter, Lisa M, Stoll, Vincent, Vasudevan, Anil, Wang, Lei, Wang, Lu, Wirthl, William, Yach, Kimberly

“…A HTS campaign identified compound 1, an excellent hit-like molecule to initiate medicinal chemistry efforts to optimize a dual ROCK1 and ROCK2 inhibitor…”
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Synthesis of ABBV-168, a 2′-Bromouridine for the Treatment of Hepatitis C by Voight, Eric A, Brown, Brian S, Greszler, Stephen N, Halvorsen, Geoff T, Zhao, Gang, Kruger, Albert W, Hartung, John, Lukin, Kirill A, Martinez, Steven R, Moschetta, Eric G, Tudesco, Michael T, Ide, Nathan D

“…ABBV-168 is a dihalogenated nucleotide under investigation for the treatment of hepatitis C virus. Three synthetic routes aimed at achieving the…”
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Synthesis and evaluation of 2′-dihalo ribonucleotide prodrugs with activity against hepatitis C virus by Chris Krueger, A., Chen, Hui-Ju, Randolph, John T., Brown, Brian S., Halvorsen, Geoff T., Heyman, Howard R., Li, Tongmei, Marvin, Christopher C., Shanley, Jason P., Voight, Eric A., Bow, Daniel A.J., Van Handel, Cecilia, Peterkin, Vincent, Carr, Robert A., Stolarik, DeAnne, Dekhtyar, Tatyana, Irvin, Michelle L., Krishnan, Preethi, Henry, Rodger F., Wagner, Rolf, DeGoey, David A.

“…[Display omitted] [Display omitted] Hepatitis C virus (HCV) nucleoside inhibitors have been a key focus of nearly 2 decades of HCV drug research due to a high…”
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Fructose-1,6-bisphosphatase Inhibitors. 1. Purine Phosphonic Acids as Novel AMP Mimics by Dang, Qun, Brown, Brian S, Liu, Yan, Rydzewski, Robert M, Robinson, Edward D, Poelje, Paul D. van, Reddy, M. Rami, Erion, Mark D

“…Inhibition of FBPase is considered a promising way to reduce hepatic gluconeogenesis and therefore could be a potential approach to treat type 2 diabetes…”
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Contributions of Central and Peripheral TRPV1 Receptors to Mechanically Evoked and Spontaneous Firing of Spinal Neurons in Inflamed Rats by McGaraughty, Steve, Chu, Katharine L, Brown, Brian S, Zhu, Chang Z, Zhong, Chengmin, Joshi, Shailen K, Honore, Prisca, Faltynek, Connie R, Jarvis, Michael F

“…Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois Submitted 15 July 2008; accepted in final…”
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Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists by Brown, Brian S., Keddy, Ryan, Zheng, Guo Zhu, Schmidt, Robert G., Koenig, John R., McDonald, Heath A., Bianchi, Bruce R., Honore, Prisca, Jarvis, Michael F., Surowy, Carol S., Polakowski, James S., Marsh, Kennan C., Faltynek, Connie R., Lee, Chih-Hung

“…A series of 1,2,3,6-tetrahydropyridyl-4-carboxamides, exemplified by 6, have been synthesized and evaluated for in vitro TRPV1 antagonist activity, and in vivo…”
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Discovery of TRPV1 antagonist ABT-116 by Brown, Brian S, Keddy, Ryan, Perner, Richard J, DiDomenico, Stanley, Koenig, John R, Jinkerson, Tammie K, Hannick, Steven M, McDonald, Heath A, Bianchi, Bruce R, Honore, Prisca, Puttfarcken, Pamela S, Moreland, Robert B, Marsh, Kennan C, Faltynek, Connie R, Lee, Chih-Hung

“…The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described. Biological studies demonstrated potent…”
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In Vitro Structure−Activity Relationship and In Vivo Characterization of 1-(Aryl)-3-(4-(amino)benzyl)urea Transient Receptor Potential Vanilloid 1 Antagonists by Perner, Richard J, DiDomenico, Stanley, Koenig, John R, Gomtsyan, Arthur, Bayburt, Erol K, Schmidt, Robert G, Drizin, Irene, Zheng, Guo Zhu, Turner, Sean C, Jinkerson, Tammie, Brown, Brian S, Keddy, Ryan G, Lukin, Kurill, McDonald, Heath A, Honore, Prisca, Mikusa, Joe, Marsh, Kennan C, Wetter, Jill M, St. George, Karen, Jarvis, Michael F, Faltynek, Connie R, Lee, Chih-Hung

“…The synthesis and structure−activity relationship of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 (TRPV1) antagonists are…”
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Bis[(para-methoxy)benzyl] phosphonate prodrugs with improved stability and enhanced cell penetration by Dang, Qun, Liu, Yan, Rydzewski, Robert M., Brown, Brian S., Robinson, Edward, van Poelje, Paul D., Colby, Timothy J., Erion, Mark D.

“…A series of bis[(para-methoxy)benzyl] phosphonate esters were synthesized and evaluated as phosphonate prodrugs. Two esters ( 4b and 4c) were identified with…”
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Structure–activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists by Drizin, Irene, Gomtsyan, Arthur, Bayburt, Erol K., Schmidt, Robert G., Zheng, Guo Zhu, Perner, Richard J., DiDomenico, Stanley, Koenig, John R., Turner, Sean C., Jinkerson, Tammie K., Brown, Brian S., Keddy, Ryan G., McDonald, Heath A., Honore, Prisca, Wismer, Carol T., Marsh, Kennan C., Wetter, Jill M., Polakowski, James S., Segreti, Jason A., Jarvis, Michael F., Faltynek, Connie R., Lee, Chih-Hung

“…Novel 5,6-fused heteroaromatic ureas were synthesized and evaluated for their activity as TRPV1 antagonists. It was found that 4-aminoindoles and indazoles are…”
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5-Aminopyrazoles as Dienophiles in the Inverse Electron Demand Diels−Alder Reactions of 2,4,6-Tris(ethoxy- carbonyl)-1,3,5-triazine:  Syntheses of Pyrazolopyrimidines by Dang, Qun, Brown, Brian S, Erion, Mark D

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Gay marriage defies human nature by Brown, Brian S

“…Teachers fired, photographers fined, bakers sued, adoption licenses stripped. Because they will not worship at liberal orthodoxy's new altar: same-sex…”
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Efficient synthesis of purine analogues: an FeCl3–SiO2-promoted cyclization reaction of 4,5-diaminopyrimidines with aldehydes leading to 6,8,9-trisubstituted purines by Dang, Qun, Brown, Brian S, Erion, Mark D

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John Adams and the Spirit of Liberty by Brown, Brian S.

“…John Adams and the spirit of liberty, by C. Bradley Thompson, Lawrence: University Press of Kansas, 1998. Pp. xix + 352. $45.00 (ISBN 0-7006-0915-6)…”
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