Fu, Suhong; Xiang, Wei; Chen, Jinying; Ma, Liang; Chen, Lijuan published an article in 2017, the title of the article was Synthesis and biological evaluation of 1, 2, 4-oxadiazole derivatives as novel GPR119 agonists.Application of 596114-50-0 And the article contains the following content:
Aryloxymethyl piperidinyl 1,2,4-oxadiazoles I [R = Boc, 5-R2-2-pyrimidinyl; R1 = 5-formyl-2-furanyl, 5-formyl-2-thienyl, 5-acetyl-2-thienyl, 4-MeOC6H4, 4-MeSO2C6H4, 1-cyclopropyl-3-pyrazolyl, 1-methyl-3-pyrazolyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 2-chloro-4-pyridinyl, 6-methoxy-3-pyridinyl, 6-fluoro-3-pyridinyl, 6-methyl-3-pyridinyl, 2-pyrimidinyl, 5-pyrimidinyl, 2-pyrazinyl, 5-oxazolyl, 4-(ethoxycarbonyl)-5-methyl-2-thiazolyl, 4-(ethoxycarbonyl)-2-thiazolyl, 2-ethyl-1,2,4-oxadiazol-5-yl; R2 = Et, i-Pr, EtO] were prepared as potential GPR119 agonists; agonism of GPR119 in human cells expressing GPR119, comparison to the pos. control GSK1292263, and their calculated lipophilicities were determined The prepared compounds showed acceptable agonistic effects at GPR119; I (R = Boc; R1 = 5-pyrimidinyl) was the most active GPR119 agonist tested with an EC50 value of 20.6 nM, comparable to that of the pos. control. The structure-activity relationship of the prepared 1,2,4-oxadiazole derivatives for GPR119 agonism was determined The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Application of 596114-50-0
The Article related to butoxycarbonylpiperidinyl pyrimidinylpiperidinyl aryloxymethyl oxadiazole preparation gpr119 agonism lipophilicity, structure butoxycarbonylpiperidinyl pyrimidinylpiperidinyl aryloxymethyl oxadiazole gpr119 agonism, gpcr, gpr119, sar study, agonistic activity, camp and other aspects.Application of 596114-50-0
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia