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1.	Barlind, Jonas G, et al. (author) Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687) 2012 In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 55:23, s. 10610-10629 Journal article (peer-reviewed)abstract A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low predicted dose in man. Rational design and optimization of this series led to the discovery of compound 30 (AZD7687), which met the project objectives for potency, selectivity, in particular over ACAT1, solubility, and preclinical PK profiles. This compound showed the anticipated excellent pharmacokinetic properties in human volunteers.
2.	Plowright, Alleyn T., et al. (author) Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1 2013 In: MedChemComm. - : Royal Society of Chemistry (RSC). - 2040-2503 .- 2040-2511. ; 4:1, s. 151-158 Journal article (peer-reviewed)abstract A novel series of potent diacylglycerol acyl transferase 1 inhibitors was developed from the clinical candidate AZD3988. Replacement of the phenyl cyclohexyl-ethanoate side chain with substituted oxy-linked side chains to introduce changes in shape and polarity, reduce lipophilicity and mask the hydrogen bond donors with internal hydrogen bond acceptors led to improvements in solubility, unbound clearance and excellent selectivity over the related enzyme acyl-coenzyme A:cholesterol acyltransferase 1. A comparison of the small molecule crystal structures of compound 4 and compound 28 is described. Compounds in this series have good ADMET properties and provide an exposure-dependent decrease in circulating plasma triglyceride levels in a rat oral lipid tolerance test.

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Type of publication: journal article (2)

Type of content: peer-reviewed (2)

Author/Editor: Birch, Alan M (2); Birtles, Susan (2); Buckett, Linda K (2); Butlin, Roger J (2); Davies, Robert D M (2); Kemmitt, Paul D (2); show more...; Turnbull, Andrew V (2); Vinblad, Johanna (1); Eriksson, Jan W. (1); Nordin, Andreas (1); Barlind, Jonas G (1); Bauer, Udo A (1); Hammond, Clare D (1); Hovland, Ragnar (1); Johannesson, Petra (1); Johansson, Magnus J (1); Lindmark, Bo T (1); Morentin Gutierrez, ... (1); Noeske, Tobias A (1); O'Donnell, Charles J (1); Petersson, Annika U (1); Redzic, Alma (1); Ertan, Anne (1); Svensson, Per H. (1); Plowright, Alleyn T (1); Leach, Andrew G. (1); Barton, Peter (1); Bennett, Stuart (1); Gutierrez, Pablo Mor ... (1); Waring, Michael J. (1); show less...

University: Royal Institute of Technology (1); Uppsala University (1)

Language: English (2)

Research subject (UKÄ/SCB): Natural sciences (1)

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