Li, Fuying; Zhu, Qingzhang; Zhang, Yi; Feng, Ying; Leng, Ying; Zhang, Ao published the artcile< Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators>, Category: thiazole, the main research area is antidiabetic glucokinase activator thiazole arylacetamide derivative.
A series of N-thiazole substituted arylacetamides were designed on the basis of metabolic mechanism of the aminothiazole fragment as glucokinase (GK) activators for the treatment of type 2 diabetes. Instead of introducing a substituent to block the metabolic sensitive C-5 position on the thiazole core directly, a wide variety of C-4 or both C-4 and C-5 substitutions were explored. Compound R-9k bearing an iso-Pr group as the C-4 substituent was found possessing the highest GK activation potency with an EC50 of 0.026 μM. This compound significantly increased both glucose uptake and glycogen synthesis in rat primary cultured hepatocytes. Moreover, single oral administration of compound R-9k exerted significant reduction of blood glucose levels in both ICR and ob/ob mice. These promising results indicated that compound R-9k is a potent orally active GK activator, and is warranted for further investigation as a new anti-diabetic treatment.
Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Category: thiazole.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica