Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome.

Basic Information

ID: ALA3608212

Journal: Bioorg Med Chem Lett

Title: Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome.

Authors: Baugh SD, Pabba PK, Barbosa J, Coulter E, Desai U, Gay JP, Gopinathan S, Han Q, Hari R, Kimball SD, Nguyen HV, Ni CY, Powell DR, Smith A, Terranova KM, Wilson A, Yu XC, Lombardo VK.

Abstract: The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo activity in reducing the enzymatic activity of liver delta-5 desaturase.

CiteXplore: 26235947

DOI: 10.1016/j.bmcl.2015.07.066

Patent ID: