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Issue 4, 2017
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Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile

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Abstract

Small molecule DGAT2 inhibitors have shown promise for the treatment of metabolic diseases in preclinical models. Herein, we report the first toxicological evaluation of imidazopyridine-based DGAT2 inhibitors and show that the arteriopathy associated with imidazopyridine 1 can be mitigated with small structural modifications, and is thus not mechanism related.

Graphical abstract: Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile

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Publication details

The article was received on 12 Oct 2016, accepted on 08 Nov 2016 and first published on 22 Nov 2016


Article type: Research Article
DOI: 10.1039/C6MD00564K
Citation: Med. Chem. Commun., 2017,8, 771-779

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    Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile

    K. Futatsugi, K. Huard, D. W. Kung, J. C. Pettersen, D. A. Flynn, J. R. Gosset, G. E. Aspnes, R. J. Barnes, S. Cabral, M. S. Dowling, D. P. Fernando, T. C. Goosen, W. P. Gorczyca, D. Hepworth, M. Herr, S. Lavergne, Q. Li, M. Niosi, S. T. M. Orr, I. D. Pardo, S. M. Perez, J. Purkal, T. J. Schmahai, N. Shirai, A. M. Shoieb, J. Zhou and B. Goodwin, Med. Chem. Commun., 2017, 8, 771
    DOI: 10.1039/C6MD00564K

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