Zobrazeno 1 - 10
of 59
pro vyhledávání: '"Sharon Sadowski"'
Autor:
Gary G. Chicchi, Paul E. Finke, Joseph M. Metzger, Dorothy Levorse, Malcolm MacCoss, Margaret A. Cascieri, D. Euan MacIntyre, Laura C. Meurer, Kwei-Lan Tsao, Sharon Sadowski, Sander G. Mills
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4497-4503
An initial investigation of the novel cyclopentane scaffold 6 afforded low nanomolar human NK1 antagonists having enhanced water solubility properties compared to morpholine 1. A synthesis of this cyclopentane scaffold, having three contiguous chiral
Autor:
Madhumeeta J Dhar, Lorraine Malkowitz, Kevin T. Chapman, Kang Cheng, Steven M. Hutchins, Stephen G. Pacholok, Christopher A. Willoughby, Keith G. Rosauer, Gary G. Chicchi, David H. Weinberg, Sharon Sadowski, Smita Patel, Jerry Di Salvo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:93-96
Preparation and screening of mixture libraries based on a 2-arylindole scaffold resulted in the discovery of potent ligands for a variety of G-protein coupled receptors.
Autor:
Richard Hargreaves, D. E. Macintyre, G Mason, S Tye, E. Ber, F.D. Tattersall, Michael J Cumberbatch, J. J. Hale, Malcolm MacCoss, Margaret A. Cascieri, W. Rycroft, Paul E. Finke, Raymond G. Hill, Sharon Sadowski, David J. Williamson, Sander G. Mills
Publikováno v:
Neuropharmacology. 39:652-663
The anti-emetic profile of the novel brain penetrant tachykinin NK1 receptor antagonist MK-0869 (L-754,030) 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluor o)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine and its water soluble
Autor:
Margaret A. Cascieri, Malcolm MacCoss, Gary G. Chicchi, Gregory E. Koch, Sharon Sadowski, Stephen E. de Laszlo, Candice Hacker, E. Ber, William K. Hagmann, Pasquale P. Vicario, Donna Louizides
Publikováno v:
Journal of Biological Chemistry. 274:8694-8697
We have identified a series of potent, orally bioavailable, non-peptidyl, triarylimidazole and triarylpyrrole glucagon receptor antagonists. 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)p yrr ole (L-168,049), a prototypical member of
Autor:
P. E. Finke, Gary G. Chicchi, Nadia M.J. Rupniak, George J. Eiermann, Nancy N. Tsou, E. Ber, Angela Williams, W. Rycroft, Margaret A. Cascieri, Sander G. Mills, Richard Hargreaves, M. Maccoss, Joe Metzger, D. E. Macintyre, Myra B. Kurtz, Sharon Sadowski, J. J. Hale, F.D. Tattersall
Publikováno v:
Journal of Medicinal Chemistry. 41:4607-4614
Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluor
Autor:
Angela Williams, Raymond G. Hill, Guanghan Liu, Margaret A. Cascieri, John J. Sramek, John P. Feighner, Gary G. Chicchi, Ram K. Shrivastava, Malcolm MacCoss, Edward M. Scolnick, Duane B. Snavely, Emma J. Carlson, Louise Hewson, Christopher John Swain, Jeffrey J. Hale, Sharon Sadowski, N.R. Cutler, David D. Smith, Nadia M.J. Rupniak, Franz Hefti, Timothy Harrison, Edwina Wyatt-Knowles, Sander G. Mills, Scott A. Reines, Richard Hargreaves, John Carman, Mark S. Kramer
Publikováno v:
Science. 281:1640-1645
The localization of substance P in brain regions that coordinate stress responses and receive convergent monoaminergic innervation suggested that substance P antagonists might have psychotherapeutic properties. Like clinically used antidepressant and
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2259-2262
We report that a systematic modification of an NK1 receptor selective antagonist resulted in the identification of novel compounds, 4c and 4d, with high affinity for both NK1 and NK2 receptors.
Autor:
Myra B. Kurtz, Gary G. Chicchi, Sharon Sadowski, Graeme Irvine Stevenson, Margaret A. Cascieri, Angus Murray Macleod, Jason Matthew Elliott, Ian Thomas Huscroft, Howard B. Broughton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:1851-1856
Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.
Autor:
Timothy Harrison, Margaret A. Cascieri, Guy R. Seabrook, M. P. G. Korsgaard, Christopher John Swain, Sharon Sadowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:1343-1348
High affinity, selective hNK2 or hNK3 ligands can be prepared from the common template 1 in a few simple chemical operations. The hNK3 ligands 3 antagonise the calcium mobilisation caused by activation of hNK3 receptors expressed in CHO cells as meas
Autor:
Andrew Pate Owens, Margaret A. Cascieri, Timothy Harrison, J. D. Moseley, Christopher John Swain, Sharon Sadowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:51-56
Heterocyclic replacements for the carboxamido group of the previously disclosed phenylglycinol-based human NK1 (hNK1) receptor antagonists have been investigated, ultimately leading to acyclic compounds with sub-nanomolar affinity for the hNK1 recept