Elovl6, a member of long chain fatty acid elongase, is a microsomal enzyme, which is responsible for the elongation of  saturated and unsaturated long chain fatty acids and has an important role in regulation of lipid metabolism.  The improvement of high-fat diet induced insulin resistance in the elovl6 deficient mice suggest that elovl6 inhibitor has possibility to be a new target for the treatment of  metabolic disorders such as insuline resistance, diabetes and cardiovascular.  In this presentation, we will present the discovery of a novel series of 3-susbstituted phenylsulfamides as elovl6 inhibitors.  The details of the structure-activity relationships, DMPK profiles and the effect on the elongation index of fatty acids (C16/C18 ration) in mice liver will be discussed.

Discovery of aryl sulfamides as elovl-6 inhitibors

245th National Meeting (2013)

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