Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Nigel E. Austin"'
Autor:
Ann Vos, Frederik Jan Rita Rombouts, Andrés A. Trabanco, Daniel Oehlrich, Harrie J.M. Gijsen, Diederik Moechars, Sven Franciscus Anna Van Brandt, Aldo Peschiulli, Gregor James Macdonald, Michel Surkyn, Gary Tresadern, Michiel Van Gool, Nigel E. Austin, Michel Anna Jozef De Cleyn
Publikováno v:
ACS Med Chem Lett
[Image: see text] We recently disclosed a set of heteroaryl-fused piperazine inhibitors of BACE1 that combined nanomolar potency with good intrinsic permeability and low Pgp-mediated efflux. Herein we describe further work on two prototypes of this f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1a245817121859b9f393819774f0f13
https://doi.org/10.1021/acsmedchemlett.1c00445
https://doi.org/10.1021/acsmedchemlett.1c00445
Autor:
Yasuyoshi Iso, Naoki Kanegawa, Vijay Urmaliya, Kazuki Fujimoto, Kazuo Komano, Ard Teisman, An Van Den Bergh, Herman Borghys, Hisanori Ito, Shuhei Yoshida, Shigeru Ando, Yasuto Kido, Nigel E. Austin, Naoya Asada, Shinji Suzuki, Kenji Nakahara, Ken-ichi Kusakabe, Eriko Matsuoka, Harrie J.M. Gijsen, Gaku Sakaguchi, Genta Tadano, Yoshinori Yamano, Tamio Fukushima, Takahiko Yamamoto, Deborah Dhuyvetter, Kouki Fuchino
Publikováno v:
Journal of medicinal chemistry. 62(20)
Genetic evidence points to deposition of amyloid-β (Aβ) as a causal factor for Alzheimer's disease. Aβ generation is initiated when β-secretase (BACE1) cleaves the amyloid precursor protein. Starting with an oxazine lead 1, we describe the discov
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b57fbfca1a3d2a869316fa567c087260
https://pubmed.ncbi.nlm.nih.gov/31549838
https://pubmed.ncbi.nlm.nih.gov/31549838
Autor:
Neil Upton, Tania O. Stean, Claire Roberts, Michael S. Hadley, Vicky Holland, Gary W. Price, Laurie J. Gordon, Jeannette M. Watson, Jenifer Powles, Claire M. Scott, Leanne Cutler, Tanya Coleman, Tom D. Heightman, Andrew Ayrton, Jean-Pierre Pilleux, Sarah L. Pardoe, Graham J. Riley, Laramie Mary Gaster, Nigel E. Austin, Brenda K. Trail, Derek N. Middlemiss
The novel 8-piperazinyl-2,3-dihydropyrroloisoquinoline template was synthesized in nine steps. The template was N-substituted to give a series of compounds showing binding to human cloned 5-HT1A, 5-HT1B and 5-HT1D receptors with pKi’s greater than
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86421f00e16772e71fb543436a7895c9
https://doi.org/10.1016/j.bmcl.2005.06.042
https://doi.org/10.1016/j.bmcl.2005.06.042
Autor:
Adam J. Lucas, Filippo Andreetta, Kevin D. Read, Declan N.C. Jones, Charles H. Large, Andrea M. Bradford, Simon T. Bate, Ilaria Sartori, Silvia Bison, Nigel E. Austin, Giuseppe Alvaro, Nicoletta Garbati, Mikhail Kalinichev
Publikováno v:
Epilepsia. 51:1543-1551
Summary Purpose: Many patients with epilepsy are refractory to anticonvulsant drugs or do not tolerate side effects associated with the high doses required to fully prevent seizures. Antagonists of neurokinin-1 (NK1) receptors have the potential to r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dcf8375253ccd4cd42fb824b898d1fac
https://doi.org/10.1111/j.1528-1167.2009.02482.x
https://doi.org/10.1111/j.1528-1167.2009.02482.x
Autor:
Andrea M. Bradford, Adam J. Lucas, Alberto Ruffo, Kevin D. Read, Nigel E. Austin, Giuseppe Alvaro, Mikhail Kalinichev, Corrado Carignani, Charles H. Large, Declan N.C. Jones, Ilaria Sartori, Nicoletta Garbati
Publikováno v:
Epilepsy Research. 85:96-106
The development of novel anticonvulsant drugs with improved efficacy for the treatment of epilepsy is hindered by a lack of information regarding the quantitative relationship between target mechanism and in vivo efficacy. In the present study we hav
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5da82e2b0be24a1ca5e28704e1466ef
https://doi.org/10.1016/j.eplepsyres.2009.02.018
https://doi.org/10.1016/j.eplepsyres.2009.02.018
Autor:
Ceri H. Davies, Adrianna Teriakidis, Anita K. Roopun, James N.C. Kew, Andrew D. Randall, Zining Wu, Hugh J. Herdon, Jon T. Brown, Ross Jeggo, Nisha Patel, Ian Thomson Forbes, Clive Leslie Branch, Gareth A. Jones, Miles A. Whittington, Victoria Anne Honey Fry, Nigel E. Austin, Martyn D. Wood, Rosemary A. Melarange, Katherine A. Buchanan, Joanne Pardoe, Christopher J. Langmead, Claire Roberts, Kathryn R. Starr, Angelica Mazzali, Jeannette M. Watson, Jim J. Hagan
Publikováno v:
British Journal of Pharmacology. 154:1104-1115
Background and purpose: M1 muscarinic ACh receptors (mAChRs) represent an attractive drug target for the treatment of cognitive deficits associated with diseases such as Alzheimer's disease and schizophrenia. However, the discovery of subtype-selecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dac8abe64a3e1b5579239d947761bc06
https://doi.org/10.1038/bjp.2008.152
https://doi.org/10.1038/bjp.2008.152
Autor:
Peter R. Maycox, Nigel E. Austin, Melanie J. Robbins, Susan H. Moore, Kevin M. Savage, Declan N.C. Jones, Mikhail Kalinichev, Elizabeth M. Hartfield
Publikováno v:
Progress in Neuro-Psychopharmacology and Biological Psychiatry. 32:414-422
In a putative model of acute phencyclidine (PCP)-induced psychosis we evaluated effects of the drug on locomotor activity (LMA) and immediate early gene (IEG) induction in the rat using two routes of drug administration, intraperitoneal (i.p.) and su
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::015295807724ef58fedb0fb1ad70e325
https://doi.org/10.1016/j.pnpbp.2007.09.008
https://doi.org/10.1016/j.pnpbp.2007.09.008
Autor:
Phillip Jeffrey, Jeannette M. Watson, Charles R. Ashby, Alexander Baxter Smith, Gregor James Macdonald, Geoffrey Stemp, Chris Johnson, David John SmithKline Beecham Pharmaceut. Nash, Clive Leslie GlaxoSmithKline Branch, Izzy Boyfield, Kevin Michael Harlow Thewlis, Kim Y. Winborn, Charlie Reavill, Riley Gj, Antonio Kuok K.łSmithKline Beecham P Vong, Jim J. Hagan, Michael Stewart Beecham Pharmaceuticals Hadley, Steve Parker, Nigel E. Austin, Derek N. Middlemiss, Martyn Wood
Publikováno v:
Journal of Medicinal Chemistry. 46:4952-4964
At their clinical doses, current antipsychotic agents share the property of both dopamine D(2) and D(3) receptor blockade. However, a major disadvantage of many current medications are the observed extrapyramidal side-effects (EPS), postulated to ari
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46d6ed3b6b25d7dfcb46b55858bd9def
https://doi.org/10.1021/jm030817d
https://doi.org/10.1021/jm030817d
Autor:
Martyn C. Coldwell, Jeffrey C. Jerman, Wai N. Chan, Phillip Jeffrey, Roderick A. Porter, Amanda Johns, Widdowson Katherine L, Nigel E. Austin, F Jewitt, Darren Smart, Steven Coulton, Michael S. Hadley, Stephen J. Brough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1907-1910
This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quinolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (SB-334867), has excellent selectivity for the orexin-1 receptor, blood-brain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e603ea593060555151d534b4cadea8d
https://doi.org/10.1016/s0960-894x(01)00343-2
https://doi.org/10.1016/s0960-894x(01)00343-2
Autor:
Gregor James Macdonald, Phillip Jeffrey, Nigel E. Austin, Vong Antonio Kuok Keong, Graham J. Riley, Izzy Boyfield, Christopher N. Johnson, Alexander Baxter Smith, Clive Leslie Branch, Geoffrey Stemp, Kim Y. Avenell, Michael S. Hadley, Kevin M. Thewlis, Martyn D. Wood, David John Nash
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:685-688
Starting from the tetrahydroisoquinoline SB-277011 1, a novel series of 5-substituted-2,3-dihydro-1H-isoindoles has been designed. Subsequent optimisation resulted in identification of 19, which has high affinity for the dopamine D3 receptor (pKi 8.3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48ececfdc04651e6149733a9695bddb3
https://doi.org/10.1016/s0960-894x(01)00037-3
https://doi.org/10.1016/s0960-894x(01)00037-3