Okazaki, Shogo; Noguchi-Yachide, Tomomi; Sakai, Taki; Ishikawa, Minoru; Makishima, Makoto; Hashimoto, Yuichi; Yamaguchi, Takao published the artcile< Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonistic activity>, Reference of 401567-00-8, the main research area is phenoxyphenyloxadiazolylethylacetamide acetyl CoA carboxylase ACC2 inhibitor PPAR agonist; Acetyl-CoA carboxylase; Multi-target drug; Peroxisome proliferator-activated receptor.
Acetyl-Co-A carboxylases (ACCs) catalyze a critical step in de novo lipogenesis, and are considered as promising targets for treatment of obesity, dyslipidemia and type 2 diabetes mellitus. On the other hand, peroxisome proliferator-activated receptors (PPARs) are well-established therapeutic targets for these metabolic syndrome-related diseases. Therefore, the authors considered that dual modulators of ACC and PPARs would be promising candidates as therapeutic agents. Here, the authors designed a series of acetamides based on the mol. similarity between ACC inhibitors and PPAR agonists. Screening of the synthesized compounds identified N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel ACC2 inhibitors with PPARα/PPARδ dual agonistic activity. Structure-activity relationship studies and further structural elaboration afforded compounds with distinct activity profiles. The findings should be helpful for the discovery of candidate agents with an appropriate balance of ACC-inhibitory and PPAR-activating activities for therapeutic lipid control.
Bioorganic & Medicinal Chemistry published new progress about Homo sapiens. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, Reference of 401567-00-8.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem