Search Results - "Koble, Cecilia"

The Naphthyridinone GSK364735 Is a Novel, Potent Human Immunodeficiency Virus Type 1 Integrase Inhibitor and Antiretroviral by GARVEY, Edward P, JOHNS, Brian A, WEATHERHEAD, Jason G, KOBLE, Cecilia S, ALIEN, Scott H, SCHALLER, Lee T, SHERRILL, Ronald G, YOSHINAGA, Tomokazu, KOBAYASHI, Masanori, WAKASA-MORIMOTO, Chiaki, MIKI, Shigeru, NAKAHARA, Koichiro, GARTLAND, Margaret J, NOSHI, Takeshi, SATO, Akihiko, FUJIWARA, Tamio, FOSTER, Scott A, MILLER, Wayne H, FERRIS, Robert G, HAZEN, Richard J, UNDERWOOD, Mark R, BOROS, Eric E, THOMPSON, James B

“…ERRATUM ( vol. 52 , p. 1899 ) Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg…”
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Novel 4,4-Disubstituted Piperidine-Based C–C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile by Kazmierski, Wieslaw M, Anderson, Don L, Aquino, Christopher, Chauder, Brian A, Duan, Maosheng, Ferris, Robert, Kenakin, Terrence, Koble, Cecilia S, Lang, Dan G, Mcintyre, Maggie S, Peckham, Jennifer, Watson, Christian, Wheelan, Pat, Spaltenstein, Andrew, Wire, Mary B, Svolto, Angilique, Youngman, Michael

“…We recently described ( J. Med. Chem. 2008, 51, 6538−6546 ) a novel class of CCR5 antagonists with strong anti-HIV potency. Herein, we detail SAR converting…”
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Naphthyridinone (NTD) integrase inhibitors: N1 Protio and methyl combination substituent effects with C3 amide groups by Johns, Brian A., Kawasuji, Takashi, Weatherhead, Jason G., Boros, Eric E., Thompson, James B., Koble, Cecilia S., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Fujiwara, Tamio

“…Substituent effects of a series of N1 protio and methyl naphthyridinone HIV-1 integrase strand-transfer inhibitors has been explored. The effects of…”
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Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups by Johns, Brian A., Kawasuji, Takashi, Weatherhead, Jason G., Boros, Eric E., Thompson, James B., Koble, Cecilia S., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Fujiwara, Tamio

“…A series of N1 acetamide substituted naphthyridinone HIV-1 integrase inhibitors have been explored to understand structure–activity relationships (SAR) with…”
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Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4- b]pyridin-5(4 H)-ones by Boros, Eric E., Johns, Brian A., Garvey, Edward P., Koble, Cecilia S., Miller, Wayne H.

“…HIV integrase strand transfer IC 50 range = 151–0.03 μM. An efficient synthesis of methyl 7-hydroxy[1,3]thiazolo[5,4- b]pyridin-5(4 H)-one-6-carboxylates ( 8–…”
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Synthesis and Antiviral Activity of 7-Benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV Integrase Inhibitors by Boros, Eric E, Edwards, Cynthia E, Foster, Scott A, Fuji, Masahiro, Fujiwara, Tamio, Garvey, Edward P, Golden, Pamela L, Hazen, Richard J, Jeffrey, Jerry L, Johns, Brian A, Kawasuji, Takashi, Kiyama, Ryuichi, Koble, Cecilia S, Kurose, Noriyuki, Miller, Wayne H, Mote, Angela L, Murai, Hitoshi, Sato, Akihiko, Thompson, James B, Woodward, Mark C, Yoshinaga, Tomokazu

“…The medicinal chemistry and structure−activity relationships for a novel series of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV-integrase inhibitors are…”
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Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the Human Immunodeficiency Virus-1 by Kazmierski, Wieslaw M, Aquino, Christopher, Chauder, Brian A, Deanda, Felix, Ferris, Robert, Jones-Hertzog, Deborah K, Kenakin, Terrence, Koble, Cecilia S, Watson, Christian, Wheelan, Pat, Yang, Hanbiao, Youngman, Michael

“…We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and…”
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Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma by Kliewer, S.A. (Glaxo Wellcome Research and Development, Research Triangle Park, NC.), Sundseth, S.S, Jones, S.A, Brown, P.J, Wisely, G.B, Koble, C.S, Devchand, P, Walhi, W, Willson, T.M, Lenhard, J.M

“…Peroxisome proliferator-activated receptors (PPARs) alpha and gamma are key regulators of lipid homeostasis and are activated by a structurally diverse group…”
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A Ureido-Thioisobutyric Acid (GW9578) Is a Subtype-Selective PPARα Agonist with Potent Lipid-Lowering Activity by Brown, Peter J, Winegar, Deborah A, Plunket, Kelli D, Moore, Linda B, Lewis, Michael C, Wilson, Joan G, Sundseth, Scott S, Koble, Cecilia S, Wu, Zhengdong, Chapman, James M, Lehmann, Jürgen M, Kliewer, Steven A, Willson, Timothy M

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A Scaleable Synthesis of Methyl 3-Amino-5-(4-fluorobenzyl)-2-pyridinecarboxylate by Boros, Eric E, Burova, Svetlana A, Erickson, Greg A, Johns, Brian A, Koble, Cecilia S, Kurose, Noriyuki, Sharp, Matthew J, Tabet, Elie A, Thompson, James B, Toczko, Matthew A

“…A scaleable synthesis of methyl 3-amino-5-(4-fluorobenzyl)-2-pyridinecarboxylate (1b), starting from 5-bromo-2-methoxypyridine (8) and 4-fluorobenzaldehyde…”
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The Naphthyridinone GSK364735 Is a Novel, Potent Human Immunodeficiency Virus Type 1 Integrase Inhibitor and Antiretroviral by Garvey, Edward P, Johns, Brian A, Gartland, Margaret J, Foster, Scott A, Miller, Wayne H, Ferris, Robert G, Hazen, Richard J, Underwood, Mark R, Boros, Eric E, Thompson, James B, Weatherhead, Jason G, Koble, Cecilia S, Allen, Scott H, Schaller, Lee T, Sherrill, Ronald G, Yoshinaga, Tomokazu, Kobayashi, Masanori, Wakasa-Morimoto, Chiaki, Miki, Shigeru, Nakahara, Koichiro, Noshi, Takeshi, Sato, Akihiko, Fujiwara, Tamio

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1-(Fluorobenzyl)-4-amino-1H-1,2,3-triazolo[4,5-c]pyridines: Synthesis and Anticonvulsant Activity by Kelley, James L, Koble, Cecilia S, Davis, Ronda G, McLean, Ed W, Soroko, Francis E, Cooper, Barrett R

“…A series of (fluorobenzyl)triazolo[4,5-c]pyridines was synthesized and tested for activity against maximal electroshock-induced seizures in rodents. The most…”
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Synthesis of Ultra-Short-Acting Neuromuscular Blocker GW 0430:  A Remarkably Stereo- and Regioselective Synthesis of Mixed Tetrahydroisoquinolinium Chlorofumarates by Samano, Vicente, Ray, John A, Thompson, James B, Mook, Robert A, Jung, David K, Koble, Cecilia S, Martin, Michael T, Bigham, Eric C, Regitz, Craig S, Feldman, Paul L, Boros, Eric E

“…The stereo- and regioselective synthesis of ultra-short-acting nondepolarizing neuromuscular blocker GW 0430 (5a) is described. Key steps involved the…”
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Neuromuscular Blocking Activity and Therapeutic Potential of Mixed-Tetrahydroisoquinolinium Halofumarates and Halosuccinates in Rhesus Monkeys by Boros, Eric E, Samano, Vicente, Ray, John A, Thompson, James B, Jung, David K, Kaldor, Istvan, Koble, Cecilia S, Martin, Michael T, Styles, Virgil L, Mook, Robert A, Feldman, Paul L, Savarese, John J, Belmont, Matthew R, Bigham, Eric C, Boswell, G. Evan, Hashim, Mir A, Patel, Sanjay S, Wisowaty, James C, Bowers, Gary D, Moseley, Caroline L, Walsh, John S, Reese, Mindy J, Rutkowske, Randy D, Sefler, Andrea M, Spitzer, Timothy D

“…Structure−activity relationships in rhesus monkeys for a novel mixed-onium class of ultra-short-acting nondepolarizing tetrahydroisoquinolinium neuromuscular…”
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Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase by Maynard, Andrew, Crosby, Renae M., Ellis, Byron, Hamatake, Robert, Hong, Zhi, Johns, Brian A., Kahler, Kirsten M., Koble, Cecilia, Leivers, Anna, Leivers, Martin R., Mathis, Amanda, Peat, Andrew J., Pouliot, Jeffrey J., Roberts, Christopher D., Samano, Vicente, Schmidt, Rachel M., Smith, Gary K., Spaltenstein, Andrew, Stewart, Eugene L., Thommes, Pia, Turner, Elizabeth M., Voitenleitner, Christian, Walker, Jill T., Waitt, Greg, Weatherhead, Jason, Weaver, Kurt, Williams, Shawn, Wright, Lois, Xiong, Zhiping Z., Haigh, David, Shotwell, J. Brad

“…A boronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and known clinical…”
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2-Acetylpyridine thiocarbonohydrazones. Potent inactivators of herpes simplex virus ribonucleotide reductase by Blumenkopf, Todd A, Harrington, Joan A, Koble, Cecilia S, Bankston, Donald D, Morrison, Robert W, Bigham, Eric C, Styles, Virgil L, Spector, Thomas

“…A series of 2-acetylpyridine thiocarbonohydrazones was synthesized for evaluation as potential antiherpetic agents. The compounds were prepared by the…”
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[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists : derivatizations at the N-terminal of the piperidine ring by MAOSHENG DUAN, AQUINO, Christopher, FERRIS, Robert, KAZMIERSKI, Wieslaw M, KENAKIN, Terry, KOBLE, Cecilia, WHEELAN, Pat, WATSON, Chris, YOUNGMAN, Michael

“…Several series of CCR5 antagonists have been discovered by derivatization at the N-terminal of the piperidine ring of the core template 2. Some derivatives…”
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Synthesis of 4‐Substituted Piperidines via a Mild and Scalable Two‐Step Cu 2 O‐Mediated Decarboxylation of Cyanoesters by Chauder, Brian A., Boros, Eric E., Du, Kien S., Kazmierski, Wieslaw M., Koble, Cecilia S., Thompson, James B., Tabet, Elie A.

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Synthesis of 4-Substituted Piperidines via a Mild and Scalable Two-Step Cu2O-Mediated Decarboxylation of Cyanoesters by Chauder, Brian A., Boros, Eric E., Du, Kien S., Kazmierski, Wieslaw M., Koble, Cecilia S., Thompson, James B., Tabet, Elie A.

“…A four-step, high-yielding, kilogram-scale protocol to prepare aldehyde 5 is reported. The key reaction is a mild, two-step Cu 2 O-mediated decarboxylation of…”
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Cis- and trans-4-n-Propyl-1,2,3,4,4a,5,6,10b-octahydrobenzo(f)quinolines by Cannon, J G, Koble-Suarez, C, Long, J P, Ilhan, M, Bhatnagar, R K

“…Cis- and trans-4-n-Propyloctahydrobenzo(f)quinolines 4a,b were prepared for further assessment of dopaminergic effects of non-oxygenated dopamine congeners…”
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