Structure and anti-acetylcholinesterase activity of 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B.
The structure of a metabolite produced on incubation of territrem B (1) with rat liver microsomes has been established to be 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B (5). Compound 5 was a potent inhibitor of electric eel acetylcholinesterase (AChE) (E.C. 3.1.1.7).
Peng
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Institute of Toxicology, College of Medicine, National Taiwan University, Taipei, Republic of China.
D000110:Acetylcholinesterase / Q000187:drug effects; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D009183:Mycotoxins / Q000737:chemistry / Q000494:pharmacology; D011714:Pyrans / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013329:Structure-Activity Relationship; D014101:Torpedo
D002800:Cholinesterase Inhibitors; D009183:Mycotoxins; D011714:Pyrans; C075495:4-hydroxymethyl-4-demethylterritrem B; D000110:Acetylcholinesterase