Search Results - "Magnin, David R."

Discovery and Preclinical Profile of Saxagliptin (BMS-477118):  A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes by Augeri, David J, Robl, Jeffrey A, Betebenner, David A, Magnin, David R, Khanna, Ashish, Robertson, James G, Wang, Aiying, Simpkins, Ligaya M, Taunk, Prakash, Huang, Qi, Han, Song-Ping, Abboa-Offei, Benoni, Cap, Michael, Xin, Li, Tao, Li, Tozzo, Effie, Welzel, Gustav E, Egan, Donald M, Marcinkeviciene, Jovita, Chang, Shu Y, Biller, Scott A, Kirby, Mark S, Parker, Rex A, Hamann, Lawrence G

“…Efforts to further elucidate structure−activity relationships (SAR) within our previously disclosed series of β-quaternary amino acid linked…”
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Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP) by Sulsky, Richard, Magnin, David R., Huang, Yanting, Simpkins, Ligaya, Taunk, Prakash, Patel, Manorama, Zhu, Yeheng, Stouch, Terry R., Bassolino-Klimas, Donna, Parker, Rex, Harrity, Thomas, Stoffel, Robert, Taylor, David S., Lavoie, Thomas B., Kish, Kevin, Jacobson, Bruce L., Sheriff, Steven, Adam, Leonard P., Ewing, William R., Robl, Jeffrey A.

“…X-ray crystal structure of an FABP inhibitor bound to the active site of aFABP. Herein we report the first disclosure of biphenyl azoles that are nanomolar…”
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A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors by Robl, Jeffrey A, Sulsky, Richard, Sun, Chong-Qing, Simpkins, Ligaya M, Wang, Tammy, Dickson, John K, Chen, Ying, Magnin, David R, Taunk, Prakash, Slusarchyk, William A, Biller, Scott A, Lan, Shih-Jung, Connolly, Fergal, Kunselman, Lori K, Sabrah, Talal, Jamil, Haris, Gordon, David, Harrity, Thomas W, Wetterau, John R

“…A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in…”
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Palladium-Catalyzed Microwave-Assisted Amination of 1-Bromonaphthalenes and 5- and 8-Bromoquinolines by Wang, Tammy, Magnin, David R, Hamann, Lawrence G

“…1-Aminonaphthalenes and 5- and 8-aminoquinolines were rapidly prepared from the respective aryl bromides in good yields by Pd-catalyzed aryl amination under…”
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Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability:  Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α-Aminoacyl-l-cis-4,5-methanoprolinenitrile-Based Inhibitors by Magnin, David R, Robl, Jeffrey A, Sulsky, Richard B, Augeri, David J, Huang, Yanting, Simpkins, Ligaya M, Taunk, Prakash C, Betebenner, David A, Robertson, James G, Abboa-Offei, Benoni E, Wang, Aiying, Cap, Michael, Xin, Li, Tao, Li, Sitkoff, Doree F, Malley, Mary F, Gougoutas, Jack Z, Khanna, Ashish, Huang, Qi, Han, Song-Ping, Parker, Rex A, Hamann, Lawrence G

“…A series of methanoprolinenitrile-containing dipeptide mimetics were synthesized and assayed as inhibitors of the N-terminal sequence-specific serine protease…”
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Regioselectivity and diastereoselectivity in free-radical macrocyclization by Porter, Ned A, Lacher, Brigitte, Chang, Vincent H. T, Magnin, David R

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Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors by Simpkins, Ligaya M., Bolton, Scott, Pi, Zulan, Sutton, James C., Kwon, Chet, Zhao, Guohua, Magnin, David R., Augeri, David J., Gungor, Timur, Rotella, David P., Sun, Zhong, Liu, Yajun, Slusarchyk, William S., Marcinkeviciene, Jovita, Robertson, James G., Wang, Aiying, Robl, Jeffrey A., Atwal, Karnail S., Zahler, Robert L., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.

“…Enzyme inhibitory activity of a series of non-nitrile dipeptides help to discern the nature of individual SAR contributions from P1 and P2 of dipeptide derived…”
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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors by Zhao, Guohua, Taunk, Prakash C., Magnin, David R., Simpkins, Ligaya M., Robl, Jeffrey A., Wang, Aiying, Robertson, James G., Marcinkeviciene, Jovita, Sitkoff, Doree F., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.

“…Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma…”
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NMR Structure of a Potent Small Molecule Inhibitor Bound to Human Keratinocyte Fatty Acid-Binding Protein by McDonnell, Patricia A, Constantine, Keith L, Goldfarb, Valentina, Johnson, Stephen R, Sulsky, Richard, Magnin, David R, Robl, Jeffrey A, Caulfield, Thomas J, Parker, Rex A, Taylor, David S, Adam, Leonard P, Metzler, William J, Mueller, Luciano, Farmer, Bennett T

“…The NMR structure is presented for compound 1 (BMS-480404) (K i = 33 (±2) nM) bound to keratinocyte fatty acid-binding protein. This article describes…”
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Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1 by Magnin, David R., Taunk, Prakash C., Robertson, James G., Wang, Aiying, Marcinkeviciene, Jovita, Kirby, Mark S., Hamann, Lawrence G.

“…The synthesis and dipeptidyl peptidase IV inhibitory activity of glycine- and alaninenitrile dipeptides are reported. A series of…”
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Application of robotics to steady state enzyme kinetics: analysis of tight-binding inhibitors of dipeptidyl peptidase IV by Wang, Aiying, Huang, Yanting, Taunk, Prakash, Magnin, David R, Ghosh, Krishnendu, Robertson, James G

“…Using available commercial robotics and instrumentation, we developed a fully automated and rigorous steady state enzyme kinetic assay for dipeptidyl peptidase…”
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Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents by Magnin, David R, Biller, Scott A, Wetterau, John, Robl, Jeffrey A, Dickson, John K, Taunk, Prakash, Harrity, Thomas W, Lawrence, R.Michael, Sun, C.-Q, Wang, Tammy, Logan, Janette, Fryszman, Olga, Connolly, Fergal, Jolibois, Kern, Kunselman, Lori

“…A series of newly synthesized phosphonate esters were evaluated for their effects on microsomal triglyceride transfer protein activity (MTP). The most potent…”
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Orally Active Squalene Synthase Inhibitors:  Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety by Dickson, John K, Biller, Scott A, Magnin, David R, Petrillo, Edward W, Hillyer, John W, Hsieh, Dolly C, Lan, Shih-Jung, Rinehart, J. Kent, Gregg, Richard E, Harrity, Thomas W, Jolibois, Kern G, Kalinowski, Stephen S, Kunselman, Lori K, Mookhtiar, Kasim A, Ciosek, Carl P

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Enantioselective Synthesis of α-Phosphono Sulfonate Squalene Synthase Inhibitors:  Chiral Recognition in the Interactions of an α-Phosphono Sulfonate Inhibitor with Squalene Synthase by Lawrence, R. Michael, Biller, Scott A, Dickson, John K, Logan, Janette V. H, Magnin, David R, Sulsky, Richard B, DiMarco, John D, Gougoutas, Jack Z, Beyer, Barbara D, Taylor, Susan C, Lan, Shih-Jung, Ciosek, Carl P, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Slusarchyk, Dorothy A

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α-Phosphonosulfonic Acids:  Potent and Selective Inhibitors of Squalene Synthase by Magnin, David R, Biller, Scott A, Chen, Ying, Dickson, John K, Fryszman, Olga M, Lawrence, R. Michael, Logan, Janette V. H, Sieber-McMaster, Ellen S, Sulsky, Richard B, Traeger, Sarah C, Hsieh, Dolly C, Lan, Shih-Jung, Rinehart, J. Kent, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Rich, Lois C, Slusarchyk, Dorothy A, Ciosek, Carl P

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1,1-Bisphosphonate Squalene Synthase Inhibitors: Interplay Between the Isoprenoid Subunit and the Diphosphate Surrogate by Magnin, David R, Dickson, John K, Logan, Janette V, Lawrence, R. Michael, Chen, Ying, Sulsky, Richard B, Ciosek, Carl P, Biller, Scott A, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Rich, Lois C, Slusarchyk, Dorothy A

“…Inhibitors of squalene synthase have the potential to be superior cholesterol-lowering agents. We previously disclosed that lipophilic 1,1-bisphosphonates I…”
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Free-radical macrocyclization-transannular cyclization by Porter, Ned A, Chang, Vincent H. T, Magnin, David R, Wright, Bruce T

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Free radical macrocyclization by Porter, Ned A, Magnin, David R, Wright, Bruce T

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An MTP Inhibitor that Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits by Wetterau, John R., Gregg, Richard E., Harrity, Thomas W., Arbeeny, Cynthia, Cap, Michael, Connolly, Fergal, Chu, Ching-Hsuen, George, Rocco J., Gordon, David A., Jamil, Haris, Jolibois, Kern G., Kunselman, Lori K., Lan, Shih-Jung, Maccagnan, Thomas J., Ricci, Beverly, Yan, Mujing, Young, Douglas, Chen, Ying, Fryszman, Olga M., Janette V. H. Logan, Musial, Christa L., Poss, Michael A., Robl, Jeffrey A., Simpkins, Ligaya M., Slusarchyk, William A., Sulsky, Richard, Taunk, Prakash, Magnin, David R., Tino, Joseph A., Lawrence, R. Michael, Dickson, John K., Biller, Scott A.

“…Patients with abetalipoproteinemia, a disease caused by defects in the microsomal triglyceride transfer protein (MTP), do not produce apolipoprotein…”
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Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo by Ciosek, C P, Magnin, D R, Harrity, T W, Logan, J V, Dickson, J K, Gordon, E M, Hamilton, K A, Jolibois, K G, Kunselman, L K, Lawrence, R M

“…Squalene synthase catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene at the final branchpoint of the cholesterol…”
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