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) inhibitorsElectronic supplementary information (ESI) available: Experimental protocols and references thereof are given. See DOI: 10.1039/c2md20231j

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 the acid with neutral isosteres. PK properties ( F...

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Hauptverfasser:	Goldberg, Frederick W, Birch, Alan M, Leach, Andrew G, Groombridge, Sam D, Snelson, Wendy L, Gutierrez, Pablo Morentin, Hammond, Clare D, Birtles, Susan, Buckett, Linda K
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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