Frkic, Rebecca L.; He, Yuanjun; Rodriguez, Beatriz B.; Chang, Mi Ra; Kuruvilla, Dana; Ciesla, Anthony; Abell, Andrew D.; Kamenecka, Theodore M.; Griffin, Patrick R.; Bruning, John B. published the artcile< Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPARγ-Targeted Antidiabetics>, Product Details of C19H34O2, the main research area is dichlorodichloroquinolinyloxyphenylbenzenesulfonamide INT131 analog preparation PPARgamma agonist antidiabetic target.
Peroxisome Proliferator-Activated Receptor γ (PPARγ) is a nuclear receptor central to fatty acid and glucose homeostasis. PPARγ is the mol. target for type 2 diabetes mellitus (T2DM) therapeutics TZDs (thiazolidinediones), full agonists of PPARγ with robust antidiabetic properties, which are confounded with significant side effects. Partial agonists of PPARγ such as INT131 (1), have displayed similar insulin-sensitizing efficacy as TZDs, but lack many side-effects. To probe the structure-activity relationship (SAR) of the scaffold (1), the authors synthesized 14 analogs of compound (1) which revealed compounds with higher transcriptional potency for PPARγ and identification of moieties of the scaffold (1) key to high transcriptional potency. The sulfonamide linker is critical to activity, substitutions at position 4 of the benzene ring A were associated with higher transcriptional activity, substitutions at position 2 aided in tighter packing and activity, and the ring type and size of ring A affected the degree of activity.
Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Product Details of C19H34O2.
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