当前位置: X-MOL 学术J. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and Characterization of Urofuranoic Acids: In Vivo Metabolism of 2-(2-Carboxyethyl)-4-methyl-5-propylfuran-3-carboxylic Acid (CMPF) and Effects on in Vitro Insulin Secretion
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-02-27 00:00:00 , DOI: 10.1021/acs.jmedchem.6b01668
Edith Nagy 1 , Ying Liu 2 , Kacey J. Prentice 2 , Kyle W. Sloop 1 , Phillip E. Sanders 1 , Battsetseg Batchuluun 2 , Craig D. Hammond 1 , Michael B. Wheeler 2 , Timothy B. Durham 1
Affiliation  

CMPF (2-(2-carboxyethyl)-4-methyl-5-propylfuran-3-carboxylic acid) is a metabolite that circulates at high concentrations in type 2 and gestational diabetes patients. Further, human clinical studies suggest it might have a causal role in these diseases. CMPF inhibits insulin secretion in mouse and human islets in vitro and in vivo in rodents. However, the metabolic fate of CMPF and the relationship of structure to effects on insulin secretion have not been significantly studied. The syntheses of CMPF and analogues are described. These include isotopically labeled molecules. Study of these materials in vivo has led to the first observation of a metabolite of CMPF. In addition, a wide range of CMPF analogues have been prepared and characterized in insulin secretion assays using both mouse and human islets. Several molecules that influence insulin secretion in vitro were identified. The molecules described should serve as interesting probes to further study the biology of CMPF.

中文翻译:

尿呋喃酸的合成与表征:2-(2-羧乙基)-4-甲基-5-丙基呋喃-3-羧酸(CMPF)的体内代谢及其对胰岛素分泌的影响

CMPF(2-(2-羧乙基)-4-甲基-5-丙基呋喃-3-羧酸)是一种代谢产物,在2型和妊娠糖尿病患者中以高浓度循环。此外,人类临床研究表明它可能在这些疾病中起因果作用。CMPF在啮齿动物中体外和体内抑制小鼠和人类胰岛中的胰岛素分泌。但是,尚未对CMPF的代谢命运以及结构与胰岛素分泌的影响之间的关系进行研究。描述了CMPF及其类似物的合成。这些包括同位素标记的分子。在体内对这些材料的研究导致首次观察到CMPF的代谢产物。另外,已经制备了多种CMPF类似物,并在使用小鼠和人胰岛的胰岛素分泌测定中对其进行了表征。鉴定了几种影响体外胰岛素分泌的分子。描述的分子应作为进一步研究CMPF生物学的有趣探针。
更新日期:2017-02-27
down
wechat
bug