CAS: 64224-60-8; 5-Bromo-4-Pyrimidinecarboxylic Acid

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1009826-93-0 114969-66-3 64224-59-5

上下游产品

CAS号21577-50-4 2,3-二溴-4-氧-2-丁烯酸 | CAS号463-52-5 formamidine | CAS号1009826-93-0 5-溴嘧啶-4-甲酸甲酯 | CAS号64224-61-9 5-甲基磺酰基嘧啶-4-羧酸乙酯

📜Mucobromic Acid,甲脒置于sodium体系中,用 乙醇 作为反应溶剂,以52%的收率获得产物5-溴-4-嘧啶甲酸
参考文献:Design,Synthesis,And Antidiabetic Activity Of 4-Phenoxynicotinamide And 4-Phenoxypyrimidine-5-Carboxamide Derivatives As Potent And Orally Efficacious Tgr5 Agonists
标题:Design,Synthesis,And Antidiabetic Activity Of 4-Phenoxynicotinamide And 4-Phenoxypyrimidine-5-Carboxamide Derivatives As Potent And Orally Efficacious Tgr5 Agonists
摘要:4-Phenoxynicotinamide And 4-Phenoxypyrimidine-5-Carboxamide Derivatives As Potent And Orally Efficacious Tgr5 Agonists Are Reported. Several 4-Phenoxynicotinamide Derivatives Were Found To Activate Human And Mouse Tgr5 (Htgr5 And Mtgr5) With Ec50 Values In The Low Nanomolar Range. Compound 23G,With An Ec50 Value Of 0.72 Nm On Htgr5 And An Ec50 Value Of 6.2 Nm On Mtgr5,Was Selected For Further In Vivo Efficacy Studies. This Compound Exhibited A Significant Dose-Dependent Glucagon-Like Peptide-1 (Glp-1) Secretion Effect. A Single Oral Dose Of 23G (50 Mg/kg) Significantly Reduced Blood Glucose Levels In Db/db Mice And Caused A 49% Reduction In The Area Under The Blood Glucose Curve (Auc)(0-120) (Min) Following An Oral Glucose Tolerance Test (Ogtt) In Imprinting Control Region (Icr) Mice. However,23G Stimulated Gallbladder Filling,Which Might Result In Side Effects To The Gallbladder.
DOI:10.1021/jm301071H