Výsledky vyhledávání - "Ashley E. Fenwick"

SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as μ opioid ligands

Autor: Graham Lunn, Lee R. Roberts, Stephane Content, Douglas J. Critcher, Sara Douglas, Ashley E. Fenwick, David M. Gethin, Graham Goodwin, David Greenway, Sean Greenwood, Kim Hall, Martin Thomas, Stephen Thompson, David Williams, Gavin Wood, Andrew Wylie

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:2200-2203

3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral μ opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting changes to the lead structure which l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c017f322826a745bdf3dc4c3c39e124b
https://doi.org/10.1016/j.bmcl.2012.01.099

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The antimicrobial natural product chuangxinmycin and Some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase

Autor: David R. Witty, Dieter Hamprecht, Ashley E. Fenwick, Paul S. Carter, Richard L. Jarvest, Murray J. B. Brown, Peter J. O'Hanlon, Martin Hibbs, Andrew J. Pope, Lucy Mensah, Christine M. Richardson, Peter Henry Milner, Andrew West, Andrew P. Fosberry

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:3171-3174

The antimicrobial natural product chuangxinmycin has been found to be a potent and selective inhibitor of bacterial tryptophanyl tRNA synthetase (WRS). A number of analogues have been synthesised. The interaction with WRS appears to be highly constra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45ff431cb2ac025b0e90504c4a1589e7
https://doi.org/10.1016/s0960-894x(02)00604-2

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3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)

Autor: Martin Saunders, Robert William Ward, Ashley E. Fenwick, Brian Peter Slingsby, Rachel Stacey, Robert John Ife, David Smith, David Haigh, Marianne Buffet

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:635-639

Potent 3-anilino-4-arylmaleimide glycogen synthase kinase-3 (GSK-3) inhibitors have been prepared using automated array methodology. A number of these are highly selective, having little inhibitory potency against more than 20 other protein kinases.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58b446377a2a20457b2c842e216cf1f9
https://doi.org/10.1016/s0960-894x(00)00721-6

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Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K

Autor: Ashley E. Fenwick, Andrew Derrick Gribble, Nichola Stevens, Jason Witherington, Robert John Ife

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:199-202

The diastereoselective synthesis of a novel class of cathepsin K inhibitors together with their cathepsin K affinity and stability towards aqueous buffer is reported.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::318fcc013b97f619587add2ef5e86c0e
https://doi.org/10.1016/s0960-894x(00)00627-2

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Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism

Autor: Michele M Gorczyca, David G. Tew, Andrew West, Patrick Lavery, Christine E. Dabrowski, Edmund J. Sternberg, Richard L. Jarvest, Ivan Leo Pinto, L.John Jennings, Ashley E. Fenwick, B. Clarke

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:449-452

Enedione derivatives of thieno[2,3-d]oxazinones are nanomolar inhibitors of CMV protease which act through a novel dual acylation of the catalytic serine and alkylation of the protease cysteine 161 via a Michael addition to the enedione moiety of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac6b4681a565a449de29591a68b2b183
https://doi.org/10.1016/s0960-894x(99)00005-0

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Endothelin-Converting Enzyme: Substrate Specificity and Inhibition by Novel Analogs of Phosphoramidon

Autor: Paul M. Keller, Walter E. DeWolf, Ashley E. Fenwick, John D. Elliott, Chao-Pin Lee, Steven Todd Atkinson

Publikováno v: Biochemical and Biophysical Research Communications. 223:372-378

Endothelin converting enzyme was partially purified by detergent extraction and ion exchange chromatography from porcine aortic endothelial cells. This kinetically homogeneous preparation catalyzes the hydrolysis of porcine big endothelin-1 to endoth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2df072bac163396ceb6d5c73ad505f9d
https://doi.org/10.1006/bbrc.1996.0901

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Inhibition of Type 4 Cyclic Nucleotide Phosphodiesterase by 8-Chloroxanthines

Autor: Brendan J. Connolly, Jonathan R. S. Arch, Ashley E. Fenwick, Harshad Kantilal Rami, Mark S. Smallridge, Derek R. Buckle, Kenneth J. Murray, Smith David Glynn, Andrew Faller

Publikováno v: Archiv der Pharmazie. 329:205-208

In an endeavour to develop isoenzyme selective inhibitors of the cyclic nucleotide phosphodiesterases, structural modifications of 8-amino-1,3-bis(cyclopropylmethyl)xanthine (BRL 61063) have been investigated. Particularly significant was the observa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d18382b84f2653f29dd4a00f722d4d0d
https://doi.org/10.1002/ardp.19963290406

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The synthesis of 2,2-bis(trifluoromethyl)benzopyran derivatives: A new route to an important class of potassium channel activators

Autor: Ashley E Fenwick

Publikováno v: Tetrahedron Letters. 34:1815-1818

A new route to an important class of biologically active benzopyrans was developed via an intramolecular cyclisation and cis diol formation.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::22798f919961722f2fc2b141f08de5b3
https://doi.org/10.1016/s0040-4039(00)60787-6

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ChemInform Abstract: Relaxant Activity of 4-Amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4- Amido-2H-1-benzopyrans on Guinea Pig Isolated Trachealis

Autor: John M. Tedder, Ashley E. Fenwick, Stephen G. Taylor, Ivan Leo Pinto, Catherine S. V. Houge-Frydrych, Jonathan R.S. Arch, Derek R. Buckle, Smith David Glynn

Publikováno v: ChemInform. 22

A series of 4-amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4-amido-2H-1-benzopyrans related to the potassium channel activator cromakalim have been prepared and evaluated for their relaxant activity in guinea pig isolated tracheal spirals. Several ana

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9af2f60dedf492916520990881fb4215
https://doi.org/10.1002/chin.199112222

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ChemInform Abstract: The Synthesis of 2,2-Bis(trifluoromethyl)benzopyran Derivatives: A New Route to an Important Class of Potassium Channel Activators

Autor: Ashley E Fenwick

Publikováno v: ChemInform. 24

A new route to an important class of biologically active benzopyrans was developed via an intramolecular cyclisation and cis diol formation.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b702808d15a2e360c93a3e42163e1dd9
https://doi.org/10.1002/chin.199330171

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