Search Results - "McBriar, Mark D."

Therapeutic potential of melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity by Kowalski, Timothy J, McBriar, Mark D

“…The compelling genetic and pharmacological evidence implicating melanin-concentrating hormone-1 receptor (MCH-1R) signalling in the regulation of food intake…”
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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 by Smith III, Amos B., Lin, Qiyan, Doughty, Victoria A., Zhuang, Linghang, McBriar, Mark D., Kerns, Jeffrey K., Brook, Christopher S., Murase, Noriaki, Nakayama, Kiyoshi

“…An advanced ABCD fragment (see picture) constructed on the way to the total synthesis of the potent antitumor agent (+)‐spongistatin 2 has also been used in a…”
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The Spongistatins: Architecturally Complex Natural Products-Part One: A Formal Synthesis of (+)-Spongistatin 1 by Construction of an Advanced ABCD Fragment by Smith III, Amos B., Doughty, Victoria A., Lin, Qiyan, Zhuang, Linghang, McBriar, Mark D., Boldi, Armen M., Moser, William H., Murase, Noriaki, Nakayama, Kiyoshi, Sobukawa, Masao

“…An advanced ABCD fragment (see picture) constructed on the way to the total synthesis of the potent antitumor agent (+)‐spongistatin 2 has also been used in a…”
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Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors by Zhao, Zhiqiang, Pissarnitski, Dmitri A., Josien, Hubert B., Bara, Thomas A., Clader, John W., Li, Hongmei, McBriar, Mark D., Rajagopalan, Murali, Xu, Ruo, Terracina, Giuseppe, Hyde, Lynn, Song, Lixin, Zhang, Lili, Parker, Eric M., Osterman, Rebecca, Buevich, Alexei V.

“…The design, synthesis, SAR, and biological profile of a substituted 4-morpholine sulfonamide series of γ-secretase inhibitors (GSIs) were described. In several…”
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Melanin concentrating hormone receptor antagonists as antiobesity agents: from M2 to MCHR-1 by McBriar, Mark D

“…Melanin concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy…”
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Discovery of Orally Efficacious Melanin-Concentrating Hormone Receptor-1 Antagonists as Antiobesity Agents. Synthesis, SAR, and Biological Evaluation of Bicyclo[3.1.0]hexyl Ureas by McBriar, Mark D, Guzik, Henry, Shapiro, Sherry, Paruchova, Jaroslava, Xu, Ruo, Palani, Anandan, Clader, John W, Cox, Kathleen, Greenlee, William J, Hawes, Brian E, Kowalski, Timothy J, O'Neill, Kim, Spar, Brian D, Weig, Blair, Weston, Daniel J, Farley, Constance, Cook, John

“…Melanin-concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy homeostasis…”
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Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors by McBriar, Mark D., Clader, John W., Chu, Inhou, Del Vecchio, Robert A., Favreau, Leonard, Greenlee, William J., Hyde, Lynn A., Nomeir, Amin A., Parker, Eric M., Pissarnitski, Dmitri A., Song, Lixin, Zhang, Lili, Zhao, Zhiqiang

“…The design of amide and heteroaryl amide isosteres as replacements for the carbamate substructure in previously disclosed 2,6-disubstituted piperidine…”
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Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2 by Smith, Amos B., Lin, Qiyan, Doughty, Victoria A., Zhuang, Linghang, McBriar, Mark D., Kerns, Jeffrey K., Boldi, Armen M., Murase, Noriaki, Moser, William H., Brook, Christopher S., Bennett, Clay S., Nakayama, Kiyoshi, Sobukawa, Masao, Lee Trout, Robert E.

“…Evolution of a convergent synthetic strategy to access (+)-spongistatin 2 ( 2), a potent cytotoxic marine macrolide, is described. Highlights of the synthesis…”
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Discovery of Bicycloalkyl Urea Melanin Concentrating Hormone Receptor Antagonists:  Orally Efficacious Antiobesity Therapeutics by McBriar, Mark D, Guzik, Henry, Xu, Ruo, Paruchova, Jaroslava, Li, Shengjian, Palani, Anandan, Clader, John W, Greenlee, William J, Hawes, Brian E, Kowalski, Timothy J, O'Neill, Kim, Spar, Brian, Weig, Blair

“…Melanin concentrating hormone (MCH) is involved in regulation of food intake and energy homeostasis. Antagonists of the MCH receptor are expected to affect…”
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Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity by Palani, Anandan, Shapiro, Sherry, McBriar, Mark D, Clader, John W, Greenlee, William J, Spar, Brian, Kowalski, Timothy J, Farley, Constance, Cook, John, van Heek, Margaret, Weig, Blair, O'Neill, Kim, Graziano, Michael, Hawes, Brian

“…Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were…”
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Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors by Li, Hongmei, Asberom, Theodros, Bara, Thomas A., Clader, John W., Greenlee, William J., Josien, Hubert B., McBriar, Mark D., Nomeir, Amin, Pissarnitski, Dmitri A., Rajagopalan, Murali, Xu, Ruo, Zhao, Zhiqiang, Song, Lixin, Zhang, Lili

“…Development of cis-2,4,6-trisubstituted piperidine N-arylsulfonamides as γ-secretase inhibitors for the potential treatment of Alzheimer’s disease (AD) is…”
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Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications by McBriar, Mark D., Guzik, Henry, Shapiro, Sherry, Xu, Ruo, Paruchova, Jaroslava, Clader, John W., O’Neill, Kim, Hawes, Brian, Sorota, Steve, Margulis, Michael, Tucker, Kristal, Weston, Daniel J., Cox, Kathleen

“…Herein, we report the discovery of an effective strategy to modulate liabilities related to affinity of previously disclosed bicyclohexane MCHR-1 antagonists…”
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Bicyclic[4.1.0]heptanes as phenyl replacements for melanin concentrating hormone receptor antagonists by Xu, Ruo, Li, Shengjian, Paruchova, Jaroslava, McBriar, Mark D., Guzik, Henry, Palani, Anandan, Clader, John W., Cox, Kathleen, Greenlee, William J., Hawes, Brian E., Kowalski, Timothy J., O’Neill, Kim, Spar, Brian D., Weig, Blair, Weston, Daniel J.

“…Bicyclic[4.1.0]heptanes were discovered as replacements for the middle phenyl ring of the biphenylamine moiety in order to eliminate its potential mutagenic…”
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Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists by Palani, Anandan, Shapiro, Sherry, McBriar, Mark D., Clader, John W., Greenlee, William J., O’Neill, Kim, Hawes, Brian

“…Herein, we report the discovery of the potent and selective biaryl diamide derived MCH-R1 receptor antagonist 1, which was identified upon modification of a…”
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Spongistatin synthetic studies. 1. Construction of a C(29–48) subtarget by Smith, Amos B., Zhuang, Linghang, Brook, Christopher S., Boldi, Armen M., McBriar, Mark D., Moser, William H., Murase, Noriaki, Nakayama, Kiyoshi, Verhoest, Patrick R., Lin, Qiyan

“…In this Letter, the first in a series of three, we outline our overall strategy and describe the assembly of a C(29–48) EF-ring advanced intermediate for the…”
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Recent advances in the discovery of melanin-concentrating hormone receptor antagonists by McBriar, Mark D

“…In recent years, obesity therapy has become a major focus of pharmaceutical research. The worldwide market for obesity therapeutics has increased dramatically…”
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The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, a NIH Postdoctoral Fellowship to C.S.B., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the by Smith III, Amos B., Lin, Qiyan, Doughty, Victoria A., Zhuang, Linghang, McBriar, Mark D., Kerns, Jeffrey K., Brook, Christopher S., Murase, Noriaki, Nakayama, Kiyoshi

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The Spongistatins: Architecturally Complex Natural Products-Part One: A Formal Synthesis of (+)-Spongistatin 1 by Construction of an Advanced ABCD Fragment Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, NIH Postdoctoral Fellowships to A.M.B. and W.H.M., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the Ta by Smith III, Amos B., Doughty, Victoria A., Lin, Qiyan, Zhuang, Linghang, McBriar, Mark D., Boldi, Armen M., Moser, William H., Murase, Noriaki, Nakayama, Kiyoshi, Sobukawa, Masao

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The Spongistatins: Architecturally Complex Natural Products-Part One: A Formal Synthesis of (+)-Spongistatin 1 by Construction of an Advanced ABCD Fragment by Smith III, Amos B., Doughty, Victoria A., Lin, Qiyan, Zhuang, Linghang, McBriar, Mark D., Boldi, Armen M., Moser, William H., Murase, Noriaki, Nakayama, Kiyoshi, Sobukawa, Masao

“…Zwei Fliegen mit einer Klappe: Bei der Totalsynthese des wirksamen Tumortherapeutikums (+)‐Spongistatin 2 wurde die komplexe ABCD‐Struktur hergestellt (siehe…”
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Spongipyran synthetic studies. Total synthesis of (+)-spongistatin 2: 2008 Tetrahedron Prize for Creativity in Organic Chemistry. The Art of Synthesis: Methods, Strategies and Applications by SMITH, Amos B, QIYAN LIN, BENNETT, Clay S, NAKAYAMA, Kiyoshi, SOBUKAWA, Masao, LEE TROUT, Robert E, DOUGHTY, Victoria A, LINGHANG ZHUANG, MCBRIAR, Mark D, KERNS, Jeffrey K, BOLDI, Armen M, MURASE, Noriaki, MOSER, William H, BROOK, Christopher S

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