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Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
McCoull W, Addie MS, Birch AM, Birtles S, Buckett LK, Butlin RJ, Bowker SS, Boyd S, Chapman S, Davies RD, Donald CS, Green CP, Jenner C, Kemmitt PD, Leach AG, Moody GC, Gutierrez PM, Newcombe NJ, Nowak T, Packer MJ, Plowright AT, Revill J, Schofield P, Sheldon C, Stokes S, Turnbull AV, Wang SJ, Whalley DP, Wood JM. McCoull W, et al. Among authors: turnbull av. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. doi: 10.1016/j.bmcl.2012.04.117. Epub 2012 May 2. Bioorg Med Chem Lett. 2012. PMID: 22608962
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J. Barlind JG, et al. Among authors: turnbull av. J Med Chem. 2012 Dec 13;55(23):10610-29. doi: 10.1021/jm301296t. Epub 2012 Nov 21. J Med Chem. 2012. PMID: 23116186
Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity.
Block MH, Boyer S, Brailsford W, Brittain DR, Carroll D, Chapman S, Clarke DS, Donald CS, Foote KM, Godfrey L, Ladner A, Marsham PR, Masters DJ, Mee CD, O'Donovan MR, Pease JE, Pickup AG, Rayner JW, Roberts A, Schofield P, Suleman A, Turnbull AV. Block MH, et al. Among authors: turnbull av. J Med Chem. 2002 Aug 1;45(16):3509-23. doi: 10.1021/jm011125x. J Med Chem. 2002. PMID: 12139462
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms.
Harno E, Cottrell EC, Yu A, DeSchoolmeester J, Gutierrez PM, Denn M, Swales JG, Goldberg FW, Bohlooly-Y M, Andersén H, Wild MJ, Turnbull AV, Leighton B, White A. Harno E, et al. Among authors: turnbull av. Endocrinology. 2013 Dec;154(12):4580-93. doi: 10.1210/en.2013-1613. Epub 2013 Oct 29. Endocrinology. 2013. PMID: 24169553 Free PMC article.
56 results