Search Results - "Noble, Stewart"

Discovery of Dual Inducible/Neuronal Nitric Oxide Synthase (iNOS/nNOS) Inhibitor Development Candidate 4-((2-Cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) Part 2: Identification of a Novel, Potent, and Selective Series of Benzimidazole-Quinolinone iNOS/nNOS Dimerization Inhibitors That Are Orally Active in Pain Models by Payne, Joseph E, Bonnefous, Céline, Symons, Kent T, Nguyen, Phan M, Sablad, Marciano, Rozenkrants, Natasha, Zhang, Yan, Wang, Li, Yazdani, Nahid, Shiau, Andrew K, Noble, Stewart A, Rix, Peter, Rao, Tadimeti S, Hassig, Christian A, Smith, Nicholas D

“…Three isoforms of nitric oxide synthase (NOS), dimeric enzymes that catalyze the formation of nitric oxide (NO) from arginine, have been identified…”
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Discovery of Inducible Nitric Oxide Synthase (iNOS) Inhibitor Development Candidate KD7332, Part 1: Identification of a Novel, Potent, and Selective Series of Quinolinone iNOS Dimerization Inhibitors that are Orally Active in Rodent Pain Models by Bonnefous, Céline, Payne, Joseph E, Roppe, Jeffrey, Zhuang, Hui, Chen, Xiaohong, Symons, Kent T, Nguyen, Phan M, Sablad, Marciano, Rozenkrants, Natasha, Zhang, Yan, Wang, Li, Severance, Daniel, Walsh, John P, Yazdani, Nahid, Shiau, Andrew K, Noble, Stewart A, Rix, Peter, Rao, Tadimeti S, Hassig, Christian A, Smith, Nicholas D

“…There are three isoforms of dimeric nitric oxide synthases (NOS) that convert arginine to citrulline and nitric oxide. Inducible NOS is implicated in numerous…”
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Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5 by Herbert, Mark R., Siegel, Dana L., Staszewski, Lena, Cayanan, Charmagne, Banerjee, Urmi, Dhamija, Sangeeta, Anderson, Jennifer, Fan, Amy, Wang, Li, Rix, Peter, Shiau, Andrew K., Rao, Tadimeti S., Noble, Stewart A., Heyman, Richard A., Bischoff, Eric, Guha, Mausumee, Kabakibi, Ayman, Pinkerton, Anthony B.

“…Optimization of a screening hit from uHTS led to the discovery of TGR5 agonist 32, which was shown to have activity in a rodent model for diabetes…”
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Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors by Pinkerton, Anthony B., Lee, Tom T., Hoffman, Timothy Z., Wang, Yan, Kahraman, Mehmet, Cook, Travis G., Severance, Daniel, Gahman, Timothy C., Noble, Stewart A., Shiau, Andrew K., Davis, Robert L.

“…We have identified and synthesized a series of thiophene containing inhibitors of kinesin spindle protein. SAR studies led to the synthesis of 33, which was…”
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Discovery of Lu AA33810: A highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder by Packiarajan, Mathivanan, Marzabadi, Mohammad R., Desai, Mahesh, Lu, Yalei, Noble, Stewart A., Wong, Wai C., Jubian, Vrej, Chandrasena, Gamini, Wolinsky, Toni D., Zhong, Hualing, Walker, Mary W., Wiborg, Ove, Andersen, Kim

“…The structure–activity relationship of a series of tricyclic-sulfonamide compounds 11–32 culminating in the discovery of…”
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Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma by Davis, Robert L., Kahraman, Mehmet, Prins, Thomas J., Beaver, Yan, Cook, Travis G., Cramp, Jessica, Cayanan, Charmagne S., Gardiner, Elisabeth M.M., McLaughlin, Marsha A., Clark, Abbot F., Hellberg, Mark R., Shiau, Andrew K., Noble, Stewart A., Borchardt, Allen J.

“…A benzothiophene containing Rho kinase inhibitor was identified in an ultra high-throughput enzymatic assay. SAR studies led to inhibitors with low nM…”
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KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo by Hassig, Christian A, Symons, Kent T, Guo, Xin, Nguyen, Phan-Manh, Annable, Tami, Wash, Paul L, Payne, Joseph E, Jenkins, David A, Bonnefous, Céline, Trotter, Carol, Wang, Yan, Anzola, John V, Milkova, Elena L, Hoffman, Timothy Z, Dozier, Sara J, Wiley, Brandon M, Saven, Alan, Malecha, James W, Davis, Robert L, Muhammad, Jerry, Shiau, Andrew K, Noble, Stewart A, Rao, Tadimeti S, Smith, Nicholas D, Hager, Jeffrey H

“…Histone deacetylase (HDAC) inhibitors have garnered significant attention as cancer drugs. These therapeutic agents have recently been clinically validated…”
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Water-soluble PDE4 inhibitors for the treatment of dry eye by Govek, Steven P., Oshiro, Guy, Anzola, John V., Beauregard, Clay, Chen, Jasmine, Coyle, Avery R., Gamache, Daniel A., Hellberg, Mark R., Hsien, Jennifer N., Lerch, Julia M., Liao, John C., Malecha, James W., Staszewski, Lena M., Thomas, David J., Yanni, John M., Noble, Stewart A., Shiau, Andrew K.

“…The development of a novel series of water-soluble PDE4 inhibitors led to the discovery of coumarin 18, which is effective in a rabbit model of dry eye and a…”
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Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors by Gahman, Timothy C., Herbert, Mark R., Lang, Henk, Thayer, Angie, Symons, Kent T., Nguyen, Phan Manh, Massari, Mark E., Dozier, Sara, Zhang, Yan, Sablad, Marciano, Rao, Tadimeti S., Noble, Stewart A., Shiau, Andrew K., Hassig, Christian A.

“…We have identified and synthesized a series of imidazole containing dimerization inhibitors of inducible nitric oxide synthase (iNOS). The necessity of key…”
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Heteroaromatic-aminomethyl quinolones: Potent and selective iNOS inhibitors by Durón, Sergio G., Lindstrom, Andrew, Bonnefous, Céline, Zhang, Hui, Chen, Xiaohong, Symons, Kent T., Sablad, Marciano, Rozenkrants, Natasha, Zhang, Yan, Wang, Li, Yazdani, Nahid, Shiau, Andrew K., Noble, Stewart A., Rix, Peter, Rao, Tadimeti S., Hassig, Christian A., Smith, Nicholas D.

“…The overproduction of nitric oxide during the biological response to inflammation by the nitric oxide synthase (NOS) enzymes have been implicated in the…”
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N-(2-Benzoylphenyl)-l-tyrosine PPARγ Agonists. 1. Discovery of a Novel Series of Potent Antihyperglycemic and Antihyperlipidemic Agents by Henke, Brad R, Blanchard, Steven G, Brackeen, Marcus F, Brown, Kathleen K, Cobb, Jeff E, Collins, Jon L, Harrington, W. Wallace, Hashim, Mir A, Hull-Ryde, Emily A, Kaldor, Istvan, Kliewer, Steven A, Lake, Debra H, Leesnitzer, Lisa M, Lehmann, Jürgen M, Lenhard, James M, Orband-Miller, Lisa A, Miller, John F, Mook, Robert A, Noble, Stewart A, Oliver, William, Parks, Derek J, Plunket, Kelli D, Szewczyk, Jerzy R, Willson, Timothy M

“…We have identified a novel series of antidiabetic N-(2-benzoylphenyl)-l-tyrosine derivatives which are potent, selective PPARγ agonists. Through the use of in…”
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KLYP956 is a non-imidazole-based orally active inhibitor of nitric-oxide synthase dimerization by Symons, Kent T, Massari, Mark E, Nguyen, Phan M, Lee, Tom T, Roppe, Jeffrey, Bonnefous, Céline, Payne, Joseph E, Smith, Nicholas D, Noble, Stewart A, Sablad, Marciano, Rozenkrants, Natasha, Zhang, Yan, Rao, Tadimeti S, Shiau, Andrew K, Hassig, Christian A

“…Nitric-oxide synthases (NOS) generate nitric oxide (NO) through the oxidation of l-arginine. Inappropriate or excessive production of NO by NOS is associated…”
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Identification of KD5170 : A novel mercaptoketone-based histone deacetylase inhibitor by PAYNE, Joseph E, BONNEFOUS, Céline, SHIAU, Andrew K, MALECHA, James W, NOBLE, Stewart A, HAGER, Jeffrey H, SMITH, Nicholas D, HASSIG, Christian A, SYMONS, Kent T, XIN GUO, NGUYEN, Phan-Manh, ANNABLE, Tami, WASH, Paul L, HOFFMAN, Timothy Z, RAO, Tadimeti S

“…We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic…”
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Pharmacological characterization of KLYP961, a dual inhibitor of inducible and neuronal nitric-oxide synthases by Symons, Kent T, Nguyen, Phan M, Massari, Mark E, Anzola, John V, Staszewski, Lena M, Wang, Li, Yazdani, Nahid, Dorow, Steven, Muhammad, Jerry, Sablad, Marciano, Rozenkrants, Natasha, Bonefous, Celine, Payne, Joseph E, Rix, Peter J, Shiau, Andrew K, Noble, Stewart A, Smith, Nicholas D, Hassig, Christian A, Zhang, Yan, Rao, Tadimeti S

“…Nitric oxide (NO) derived from neuronal nitric-oxide synthase (nNOS) and inducible nitric-oxide synthase (iNOS) plays a key role in various pain and…”
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Synthesis and Structure−Activity Relationship of Fluoro Analogues of 8-{2-[4-(4-Methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as Selective α1d-Adrenergic Receptor Antagonists by Konkel, Michael J, Wetzel, John M, Cahir, Marie, Craig, Douglas A, Noble, Stewart A, Gluchowski, Charles

“…We have discovered high-affinity antagonists (exemplified by 11 and 12) that are the most selective for α1d-adrenergic receptors (α1d-AR) reported to date. In…”
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α-Mercaptoketone based histone deacetylase inhibitors by Wash, Paul L., Hoffman, Timothy Z., Wiley, Brandon M., Bonnefous, Céline, Smith, Nicholas D., Sertic, Michael S., Lawrence, Charles M., Symons, Kent T., Nguyen, Phan-Manh, Lustig, Kevin D., Guo, Xin, Annable, Tami, Noble, Stewart A., Hager, Jeffrey H., Hassig, Christian A., Malecha, James W.

“…The identification and lead optimization of a novel series of α-mercaptoketone HDAC inhibitors is described. In an effort to discover novel non-hydroxamic acid…”
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Antisense and Antigene Properties of Peptide Nucleic Acids by Hanvey, Jeffery C., Peffer, Nancy J., Bisi, John E., Thomson, Stephen A., Cadilla, Rodolfo, Josey, John A., Ricca, Daniel J., Hassman, C. Fred, Bonham, Michele A., Au, Karin G., Carter, Stephen G., Bruckenstein, David A., Boyd, Ann L., Noble, Stewart A., Babiss, Lee E.

“…Peptide nucleic acids (PNAs) are polyamide oligomers that can strand invade duplex DNA, causing displacement of one DNA strand and formation of a D-loop…”
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An assessment of the antisense properties of RNase H-competent and steric-blocking oligomers by Bonham, Michele A., Brown, Stephen, Boyd, Ann L., Brown, Pamela H., Bruckenstein, David A., Hanvey, Jeffery C., Thomson, Stephen A., Pipe, Adrian, Hassman, Fred, Bisi, John E., Froehler, Brian C., Matteucci, Mark D., Wagner, Richard W., Noble, Stewart A., Babiss, Lee E.

“…ABSTRACT The antisense activity and gene specificity of two classes of oligonucleotides (ONs) were directly compared in a highlycontrolled assay. One class of…”
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Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines by Livermore, David G. H, Bethell, Richard C, Cammack, Nicholas, Hancock, Ashley P, Hann, Michael M, Green, Darren V. S, Lamont, R. Brian, Noble, Stewart A, Orr, David C

“…A series of substituted imidazo[1,5-b]pyridazines have been prepared and tested for inhibitory activity against the reverse transcriptase of HIV-1 (RT) and…”
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GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2 by Jones, K A, Borowsky, B, Tamm, J A, Craig, D A, Durkin, M M, Dai, M, Yao, W J, Johnson, M, Gunwaldsen, C, Huang, L Y, Tang, C, Shen, Q, Salon, J A, Morse, K, Laz, T, Smith, K E, Nagarathnam, D, Noble, S A, Branchek, T A, Gerald, C

“…The principal inhibitory neurotransmitter GABA (gamma-aminobutyric acid) exerts its effects through two ligand-gated channels, GABA(A) and GABA(C) receptors,…”
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