130778-43-7

Basic information

• Product Name: 14-hydroxyarteether
• CAS NO: 130778-43-7
• Molecular Weight: 328.406
• Mol File: 130778-43-7.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 14-hydroxyarteether(CAS DataBase Reference)
• NIST Chemistry Reference: 14-hydroxyarteether(130778-43-7)
• EPA Substance Registry System: 14-hydroxyarteether(130778-43-7)

Safety Data

• Hazardous Substances Data: 130778-43-7(Hazardous Substances Data)

Upstream product

• 75887-54-6 artemotil 

Relevant articles and documents

Synthesis, characterization, and antimalarial activity of the glucuronides of the hydroxylated metabolites of arteether

The hydroxylated metabolites (log P 2.6-2.7) of β-arteether (1) in rat liver microsomes that retain their endoperoxide moiety showed comparable in vitro antimalarial activity to that of the parent drug arteether (log P = 3.89). The search for analogs of artemisinin (7) more suitable for intravenous use led to the synthesis of the glucuronide conjugates of the phase I hydroxylated metabolites of arteether which were found to have good water solubility, yet retained moderate lipophilicity (log P = 0.6-1.8). While a strong correlation was observed between the log P value of the glucuronides, the phase I metabolites, and the parent compound, it was found that 9β-hydroxyarteetherglucuronide (26) was the most active and the most polar (log P = 0.61) of the glucuronides. While the in vitro antimalarial activity of 26 (IC50 = 89.3 ng/mL) was found to be much less than that for the parent compound, the activity of 26 was within a range that would have potential therapeutic use.