Issue 4, 2017

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

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

Supplementary files

Article information

Article type
Research Article
Submitted
12 Oct 2016
Accepted
08 Nov 2016
First published
22 Nov 2016

Med. Chem. Commun., 2017,8, 771-779

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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