Zobrazeno 1 - 10 of 11 pro vyhledávání: '"Alan Martin Birch"'
1
ACAT-selective and Nonselective DGAT1 Inhibition
Autor: Tim J.D. Smith, Alan Martin Birch, Andrew V. Turnbull, Huw B. Jones, Linda K. Buckett, Jan Eike Floettmann, Carina Hallberg, David Lees
Publikováno v: Toxicologic Pathology. 41:941-950
Acyl-coenzyme A: cholesterol O-Acyltransferase (ACAT) and Acyl-coenzyme A: diacylglycerol O-acyltransferase (DGAT) enzymes play important roles in synthesizing neutral lipids, and inhibitors of these enzymes have been investigated as potential treatm
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90aef9c324ddcb52f3eb6483b8a489bb
https://doi.org/10.1177/0192623313477753
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2
Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors
Autor: Frederick W. Goldberg, Alan Martin Birch, Andrew G. Leach, Wendy L. Snelson, Linda K. Buckett, Sam D. Groombridge, Pablo Morentin Gutierrez, Susan Birtles, Clare D. Hammond
Publikováno v: MedChemComm. 4:165-174
A series of neutral DGAT1 inhibitors with good potency and pharmacokinetics (PK) has been designed by modification of an acidic startpoint. This was achieved by selecting the acid with the highest ligand lipophilicity efficiency (LLE) and replacing t
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1b7b268fa1152bf9f3e80d035f31f2d5
https://doi.org/10.1039/c2md20231j
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3
Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists
Autor: Katy J. Brocklehurst, Paul Schofield, James S. Scott, Per H. Svensson, Sam D. Groombridge, Kristin Goldberg, Ruth Poultney, Darren Mckerrecher, Julian A. Hudson, Andrew G. Leach, Hayley S. Brown, Philip A. MacFaul, Alan Martin Birch
Publikováno v: MedChemComm. 4:95-100
Improving aqueous solubility is a challenge frequently faced within drug discovery programs. Herein we describe increases in solubility in two sub-series of GPR119 agonists through reduction of lipophilicity together with hydrogen bond acceptor modul
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e4ada7177556dab7308ef00895d296da
https://doi.org/10.1039/c2md20130e
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5
Rationally Designing Safer Anilines: The Challenging Case of 4-Aminobiphenyls
Autor: Robert P. Law, Carolin Schramm, Christine Mee, Andrew G. Leach, Sam D. Groombridge, Alan Martin Birch
Publikováno v: Journal of Medicinal Chemistry. 55:3923-3933
We describe how we have been able to design 4-aminobiphenyls that are nonmutagenic (inactive in the Ames test). No such 4-aminobiphenyls were known to us, but insights provided by quantum mechanical calculations have permitted us to design and synthe
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09cd593f22424d084b79383c6dadfe2f
https://doi.org/10.1021/jm3001295
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6
Expedient Syntheses of Sulfonylhydantoins and Two Six-Membered Analogues
Autor: Alan Martin Birch, Andrew D. Campell
Publikováno v: Synlett. :0834-0838
A range of α-amino esters can be turned into sulfonylhydantoins 2 in a single, atom-economic step using sulfamide and DBU. This procedure obviates the need for a three- or four-step sequence utilised by traditional procedures. Two new six-membered a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de8a6ea42595a8561cc88b9b0b0db8bd
https://doi.org/10.1055/s-2005-863735
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8
Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor
Autor: Steven Wang, Susan Birtles, Graham J. Smith, Linda K. Buckett, Paul D. Kemmitt, Alan Martin Birch, Tim J.D. Smith, Andrew V. Turnbull
Publikováno v: Journal of medicinal chemistry. 52(6)
Inhibition of DGAT-1 is increasingly seen as an attractive mechanism with the potential for treatment of obesity and other elements of the metabolic syndrome. We report here a bicyclooctaneacetic acid derivative in the pyrimidinooxazine structural cl
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb3ac0570eda25beff56feda0cd78789
https://pubmed.ncbi.nlm.nih.gov/19256504
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10
Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors
Autor: Paul Robert Owen Whittamore, Nikos G. Oikonomakos, Peter W. Kenny, Dave P. Whalley, Ludovic Otterbein, Paul Schofield, Alan Martin Birch
Publikováno v: Bioorganicmedicinal chemistry letters. 17(2)
A series of substituted 3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors, which have potential as antidiabetic agents, is described. Initial members of the series showed good enzyme inhibitory potency but poor physical properties. Optimisati
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97aa4d7ed4d7ff8e566967eeab6151cf
https://pubmed.ncbi.nlm.nih.gov/17095214
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