Search Results - "Newcombe, Nicholas J"

Directed Dihydroxylation of Cyclic Allylic Alcohols and Trichloroacetamides Using OsO4/TMEDA by Donohoe, Timothy J, Blades, Kevin, Moore, Peter R, Waring, Michael J, Winter, Jon J. G, Helliwell, Madeleine, Newcombe, Nicholas J, Stemp, Geoffrey

“…The oxidation of a range of cyclic allylic alcohols and amides with OsO4/TMEDA is presented. Under these conditions, hydrogen bonding control leads to the…”
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Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors by Janetka, James W., Almeida, Lynsie, Ashwell, Susan, Brassil, Patrick J., Daly, Kevin, Deng, Chun, Gero, Thomas, Glynn, Roberta E., Horn, Candice L., Ioannidis, Stephanos, Lyne, Paul, Newcombe, Nicholas J., Oza, Vibha B., Pass, Martin, Springer, Stephanie K., Su, Mei, Toader, Dorin, Vasbinder, Melissa M., Yu, Dingwei, Yu, Yan, Zabludoff, Sonya D.

“…A series of thiophene carboxamide checkpoint kinase inhibitors ( 3) were discovered through HTS and optimized for cellular potency ( 12n). Checkpoint kinase-1…”
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Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor: Discovery of 2-[(3S)-1-[5-(Cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic Acid (AZD4017) by Scott, James S, Bowker, Suzanne S, deSchoolmeester, Joanne, Gerhardt, Stefan, Hargreaves, David, Kilgour, Elaine, Lloyd, Adele, Mayers, Rachel M, McCoull, William, Newcombe, Nicholas J, Ogg, Derek, Packer, Martin J, Rees, Amanda, Revill, John, Schofield, Paul, Selmi, Nidhal, Swales, John G, Whittamore, Paul R. O

“…Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. We report here the discovery of a…”
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Identification, Optimization, and Pharmacology of Acylurea GHS-R1a Inverse Agonists by McCoull, William, Barton, Peter, Brown, Alastair J. H, Bowker, Suzanne S, Cameron, Jennifer, Clarke, David S, Davies, Robert D. M, Dossetter, Alexander G, Ertan, Anne, Fenwick, Mark, Green, Clive, Holmes, Jane L, Martin, Nathaniel, Masters, David, Moore, Jane E, Newcombe, Nicholas J, Newton, Claire, Pointon, Helen, Robb, Graeme R, Sheldon, Christopher, Stokes, Stephen, Morgan, David

“…Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are widely considered to offer…”
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A chemistry wiki to facilitate and enhance compound design in drug discovery by Robb, Graeme R., McKerrecher, Darren, Newcombe, Nicholas J., Waring, Mike J.

“…► Design and creation of a wiki-based tool for collaborative drug design. ► The tool collects data from multiple sources and summarises for different user…”
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Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes by McCoull, William, Addie, Matthew S., Birch, Alan M., Birtles, Susan, Buckett, Linda K., Butlin, Roger J., Bowker, Suzanne S., Boyd, Scott, Chapman, Stephen, Davies, Robert D.M., Donald, Craig S., Green, Clive P., Jenner, Chloe, Kemmitt, Paul D., Leach, Andrew G., Moody, Graeme C., Morentin Gutierrez, Pablo, Newcombe, Nicholas J., Nowak, Thorsten, Packer, Martin J., Plowright, Alleyn T., Revill, John, Schofield, Paul, Sheldon, Chris, Stokes, Steve, Turnbull, Andrew V., Wang, Steven J.Y., Whalley, David P., Matthew Wood, J.

“…A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand…”
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Novel 4-piperidinopyridine inhibitors of oxidosqualene cyclase-lanosterol synthase derived by consideration of inhibitor pKa by BROWN, George R, FOUBISTER, Alan J, JOHNSON, Michael C, NEWCOMBE, Nicholas J, WATERSON, David, WELLS, Stuart L

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Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors by Anderson, Malcolm, Andrews, David M., Barker, Andy J., Brassington, Claire A., Breed, Jason, Byth, Kate F., Culshaw, Janet D., Finlay, M. Raymond V., Fisher, Eric, McMiken, Helen H.J., Green, Clive P., Heaton, Dave W., Nash, Ian A., Newcombe, Nicholas J., Oakes, Sandra E., Pauptit, Richard A., Roberts, Andrew, Stanway, Judith J., Thomas, Andrew P., Tucker, Julie A., Walker, Mike, Weir, Hazel M.

“…The SAR and development of an imidazole series ( 3) of CDK inhibitors are reported. An imidazole series of cyclin-dependent kinase (CDK) inhibitors has been…”
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Carbohydrate-based enolates as heterocyclic building blocks. Synthesis of the herbicidin glycoside by Newcombe, Nicholas J, Mahon, Mary F, Molloy, Kieran C, Alker, David, Gallagher, Timothy

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The directed dihydroxylation of allylic alcohols by Donohoe, Timothy J., Moore, Peter R., Waring, Michael J., Newcombe, Nicholas J.

“…The preparation and dihydroxylation of a series of polyenes and cyclic allylic alcohols using the TMEDA/osmium tetroxide mixture is reported. Remarkably, these…”
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Homoallylic alcohols and trichloroacetamides as hydrogen bond donors for directed dihydroxylation by Donohoe, Timothy J, Mitchell, Lee, Waring, Michael J, Helliwell, Madeleine, Bell, Andrew, Newcombe, Nicholas J

“…The synthesis and directed dihydroxylation of a series of homoallylic alcohols and trichloroacetamides is described. Using the combination of OsO 4 and TMEDA,…”
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syn stereocontrol in the directed dihydroxylation of acyclic allylic alcohols by Donohoe, Timothy J., Newcombe, Nicholas J., Waring, Michael J.

“…The preparation and directed dihydroxylation of a series of acyclic allylic alcohols is reported. The oxidation reaction is capable of demonstrating high…”
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2-Keto sugars as preformed heterocyclic building blocks. Synthetic studies by GRIFFIN, A. M, NEWCOMBE, N. J, ALKER, D, RAMSAY, M. V. J, GALLAGHER, T

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The synthesis of (+)-pericosine B by Donohoe, Timothy J., Blades, Kevin, Helliwell, Madeleine, Waring, Michael J., Newcombe, Nicholas J.

“…The first synthesis of (+)-pericosine B is described: this takes seven steps and proceeds in 10% overall yield. The key step in our work is a hydrogen-bonding…”
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Directed Dihydroxylation of Cyclic Allylic Alcohols and Trichloroacetamides Using OsO 4 /TMEDA by Donohoe, Timothy J., Blades, Kevin, Moore, Peter R., Waring, Michael J., Winter, Jon J. G., Helliwell, Madeleine, Newcombe, Nicholas J., Stemp, Geoffrey

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Novel 4-piperidinopyridine inhibitors of oxidosqualene cyclase-lanosterol synthase derived by consideration of inhibitor p Ka by Brown, George R, Foubister, Alan J, Johnson, Michael C, Newcombe, Nicholas J, Waterson, David, Wells, Stuart L

“…Potent inhibition of rat microsomal oxidosqualene cyclase-lanosterol synthase (OSC) was maintained after structural modification of the 4-piperidinopyridine…”
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N-acyliminium ion cyclisations in natural product chemistry: Synthesis of gelsemine by Speckamp, W. N., Newcombe, N. J., Hiemstra, Henk, Ya, Fang, Vijn, R. J., Koot, W.-J.

“…Abstract…”
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