pig liver microsomes

• 英文名称: pig liver microsomes

反应信息

• 作为试剂：
  描述：

  佐拉沙坦 、 uridine-5'-diphospho-α-D-glucuronic acid trisodium salt 在 pig liver microsomes 作用下， 反应 7.0h， 以4.3%的产率得到zolarsartan-O-glucuronide
  参考文献：
  名称：

  Enzyme-assisted synthesis and structure characterization of glucuronic acid conjugates of losartan, candesartan, and zolarsartan

  摘要：

  Three angiotensin II receptor antagonists-losartan, candesartan, and zolarsartan-were investigated. All the compounds, which are structural analogues, are metabolized via conjugation to glucuronic acid. Interestingly, both O- and N-glucuronidation take place, so that regioisomers are formed. One ether O-glucuronide, two acyl O-glucuronides, and five tetrazole-N-glucuronides were biosynthesized, in milligram scale, from the three sartan aglycones. Liver microsomes from bovine, moose, rat, and pig and recombinant human UDP-glucuronosyltransferases were used as catalysts. The synthesized compounds were identified as sartan glucuronides by mass spectrometry, while the sites of glucuronidation were determined by nuclear magnetic resonance spectroscopy. Drug metabolites are needed as standards for pharmaceutical research and, as the present study shows, they can easily be produced with enzymes as catalyst. (C) 2008 Elsevier Inc. All rights reserved.

  DOI：

  10.1016/j.bioorg.2008.02.004