Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Nigel Austin"'
Autor:
Fazeeda N. Hosein, Nigel Austin, Shobha Maharaj, Winston Johnson, Luke Rostant, Amanda C. Ramdass, Sephra N. Rampersad
Publikováno v:
Ecology and Evolution, Vol 7, Iss 18, Pp 7311-7333 (2017)
Abstract The islands of the Caribbean are considered to be a “biodiversity hotspot.” Collectively, a high level of endemism for several plant groups has been reported for this region. Biodiversity conservation should, in part, be informed by taxo
Externí odkaz:
https://doaj.org/article/2c05f3e020794d0f96c6bcbc0f9fd392
Autor:
Ahmed Mamai, Anh M. Chau, Brian J. Wilson, Iain D. Watson, Babu B. Joseph, Pandiaraju R. Subramanian, Monzur M. Morshed, Justin A. Morin, Michael A. Prakesch, Tianbao Lu, Pete Connolly, Douglas A. Kuntz, Neil C. Pomroy, Gennady Poda, Kong Nguyen, Richard Marcellus, Graig Strathdee, Brigitte Theriault, Ratheesh Subramaniam, Mohammed Mohammed, Ayome Abibi, Manuel Chan, Jeffrey Winston, Taira Kiyota, Elijus Undzys, Ahmed Aman, Nigel Austin, Marc Du Jardin, Kathryn Packman, Ulrike Phillippar, Riccardo Attar, James Edwards, Jeff O’Meara, David E. Uehling, Rima Al-awar, Gilbert G. Privé, Methvin B. Isaac
Publikováno v:
ACS Medicinal Chemistry Letters. 14:199-210
Autor:
Ann Vos, Lieve Lammens, Richard Alexander, Frederik J. R. Rombouts, Michel Surkyn, Kenji Morimoto, Laurent Leclercq, Nigel Austin, Koichi Tsubone, Tatsuhiko Ueno, Michel Anna Jozef De Cleyn, Deborah Dhuyvetter, Ken-ichi Kusakabe, Ard Teisman, Diederik Moechars, Tom Jacobs, An Van Den Bergh, Hirokazu Sumiyoshi, Herman Borghys, Shunsuke Einaru, Soufyan Jerhaoui, Brian Joel Hrupka, Harrie J.M. Gijsen
Publikováno v:
Journal of Medicinal Chemistry. 64:14175-14191
The discovery of a novel 2-aminotetrahydropyridine class of BACE1 inhibitors is described. Their pKa and lipophilicity were modulated by a pending sulfonyl group, while good permeability and brain penetration were achieved via intramolecular hydrogen
Autor:
Yasuyoshi Iso, Shigeru Ando, Harrie J.M. Gijsen, Yasuto Kido, Shinji Suzuki, Herman Borghys, Kenji Morimoto, Vijay Urmaliya, Deborah Dhuyvetter, Takahiko Yamamoto, Ard Teisman, Gaku Sakaguchi, Naoki Kanegawa, Nigel Austin, Eriko Matsuoka, An Van Den Bergh, Hisanori Ito, Takuya Oguma, Francois Paul Bischoff, Tamio Fukushima, Peter Verboven, Tomoyuki Kawachi, Kenji Nakahara, Yoshinori Yamano, Kosuke Anan, Ken-ichi Kusakabe
Publikováno v:
ChemMedChem. 14:1894-1910
The β-site amyloid precursor protein cleaving enzyme 1 (BACE1, also known as β-secretase) is a promising target for the treatment of Alzheimer's disease. A pKa lowering approach over the initial leads was adopted to mitigate hERG inhibition and P-g
Autor:
Julia J. Schubert, Mattia Veronese, Tim D. Fryer, Roido Manavaki, Manfred G. Kitzbichler, Maria A. Nettis, Valeria Mondelli, Carmine M. Pariante, Edward T. Bullmore, Federico E. Turkheimer, Dominika Wlazly, Amber Dickinson, Andy Foster, Clare Knight, Claire Leckey, Paul Morgan, Angharad Morgan, Caroline O'Hagan, Samuel Touchard, Shahid Khan, Phil Murphy, Christine Parker, Jai Patel, Jill Richardson, Paul Acton, Nigel Austin, Anindya Bhattacharya, Nick Carruthers, Peter de Boer, Wayne Drevets, John Isaac, Declan Jones, John Kemp, Hartmuth Kolb, Jeff Nye, Gayle Wittenberg, Gareth Barker, Anna Bogdanova, Heidi Byrom, Diana Cash, Annamaria Cattaneo, Daniela Enache, Tony Gee, Caitlin Hastings, Melisa Kose, Giulia Lombardo, Nicole Mariani, Anna McLaughlin, Maria Nettis, Naghmeh Nikkheslat, Carmine Pariante, Karen Randall, Julia Schubert, Luca Sforzini, Hannah Sheridan, Camilla Simmons, Nisha Singh, Federico Turkheimer, Vicky Van Loo, Marta Vicente Rodriguez, Toby Wood, Courtney Worrell, Zuzanna Zajkowska, Brian Campbell, Jan Egebjerg, Hans Eriksson, Francois Gastambide, Karen Husted Adams, Ross Jeggo, Thomas Moeller, Bob Nelson, Niels Plath, Christian Thomsen, Jan Torleif Pederson, Stevin Zorn, Catherine Deith, Scott Farmer, John McClean, Andrew McPherson, Nagore Penandes, Paul Scouller, Murray Sutherland, Mary Jane Attenburrow, Jithen Benjamin, Helen Jones, Fran Mada, Akintayo Oladejo, Katy Smith, Rita Balice-Gordon, Brendon Binneman, James Duerr, Terence Fullerton, Veeru Goli, Zoe Hughes, Justin Piro, Tarek Samad, Jonathan Sporn, Liz Hoskins, Charmaine Kohn, Lauren Wilcock, Franklin Aigbirhio, Junaid Bhatti, Ed Bullmore, Sam Chamberlain, Marta Correia, Anna Crofts, Tim Fryer, Martin Graves, Alex Hatton, Manfred Kitzbichler, Mary-Ellen Lynall, Christina Maurice, Ciara O'Donnell, Linda Pointon, Peter St George Hyslop, Lorinda Turner, Petra Vertes, Barry Widmer, Guy Williams, Jonathan Cavanagh, Alison McColl, Robin Shaw, Erik Boddeke, Alison Baird, Stuart Clare, Phil Cowen, I-Shu (Dante) Huang, Sam Hurley, Simon Lovestone, Alejo Nevado-Holgado, Elena Ribe, Anviti Vyas, Laura Winchester, Madeleine Cleal, Diego Gomez-Nicola, Renzo Mancuso, Hugh Perry, Mara Cercignani, Charlotte Clarke, Alessandro Colasanti, Neil Harrison, Rosemary Murray, Jason O'Connor, Howard Mount
Publikováno v:
Biological Psychiatry. Cognitive Neuroscience and Neuroimaging
Background: Immune mechanisms have been implicated in the pathogenesis of depression. Translocator protein (TSPO)–targeted positron emission tomography (PET) has been used to assess neuroinflammation in major depressive disorder. We aimed to 1) tes
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2204ff869f9b3d8a8b56521d5dd1f9c9
http://hdl.handle.net/11577/3411540
http://hdl.handle.net/11577/3411540
Autor:
Sergio A. Alonso de Diego, Daniel Oehlrich, Harrie J.M. Gijsen, Andrés A. Trabanco, Hana Prokopcová, Nigel Austin, Michel Surkyn, Dries Van den Bossche, Frederik J. R. Rombouts, Deborah Dhuyvetter, Gregor James Macdonald, Sven Franciscus Anna Van Brandt, Herman Borghys, Michiel Van Gool, Diederik Moechars, Aránzazu García-Molina, Michel Anna Jozef De Cleyn, Carolina Martinez-Lamenca
Publikováno v:
Journal of Medicinal Chemistry. 61:5292-5303
In previous studies, the introduction of electron withdrawing groups to 1,4-oxazine BACE1 inhibitors reduced the pKa of the amidine group, resulting in compound 2 that showed excellent in vivo efficacy, lowering Aβ levels in brain and CSF. However,
Autor:
Mark E. Schmidt, Rhys Salter, Cindy Wintmolders, Nigel Austin, Vladimir Chupakhin, Gregor James Macdonald, Astrid Bottelbergs, Paula te Riele, Lu Chen, Katleen Fierens, Diederik Moechars, Andrés A. Trabanco, José-Ignacio Andrés, José Manuel Alonso, Jonas Mariën, Erna Cleiren, Martinez Lamenca Carolina, Frederik J. R. Rombouts, Manuela Ariza, Leenaerts Joseph Elisabeth, Xavier Langlois, Wei Zhang, Alberto Fontana
Publikováno v:
Journal of Medicinal Chemistry. 60:1272-1291
A mini-HTS on 4000 compounds selected using 2D fragment-based similarity and 3D pharmacophoric and shape similarity to known selective tau aggregate binders identified N-(6-methylpyridin-2-yl)quinolin-2-amine 10 as a novel potent binder to human AD a
Publikováno v:
Journal of Experimental Marine Biology and Ecology. 485:94-101
Mitochondrial DNA control region haplotypes of immature hawksbills feeding in Tobago waters and adult females nesting on the beaches of Tobago were characterized. Eleven haplotypes were documented among foraging aggregations and six haplotypes among
Autor:
Sven Franciscus Anna Van Brandt, Aldo Peschiulli, Andrés A. Trabanco, Ann Vos, Nigel Austin, Sergio A. Alonso de Diego, Michel Anna Jozef De Cleyn, Hana Prokopcová, Michel Surkyn, Dieder Moechars, Daniel Oehlrich, Gregor James Macdonald, Frederik J. R. Rombouts, Juan Antonio Vega, Michiel Van Gool, Ana Isabel de Lucas, Harrie J.M. Gijsen, Gary Tresadern
Publikováno v:
ACS Med Chem Lett
[Image: see text] Despite several years of research, only a handful of β-secretase (BACE) 1 inhibitors have entered clinical trials as potential therapeutics against Alzheimer’s disease. The intrinsic basic nature of low molecular weight, amidine-
Autor:
Garrett Berlond Minne, Michel Surkyn, Harrie J.M. Gijsen, Francois Paul Bischoff, Nigel Austin, Marc Mercken, Didier Berthelot, Chiara Zavattaro, Ishtiyaque Ahmad, Gregor James Macdonald, Adriana Ingrid Velter, Michel Anna Jozef De Cleyn, Deborah Dhuyvetter, Sven Franciscus Anna Van Brandt, Serge Maria Aloysius Pieters, Yves Emiel Maria Van Roosbroeck, Swapan Kumar Samanta, Herman Borghys
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(14)
The discovery, design and synthesis of a new series of GSMs is described. The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus. The exploration of this series has led to compound 26-S which combined hig