Synthesis and biological activity of the metabolites of diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate (NO-1886).
Five metabolites of diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate (NO-1886) (1) were synthesized to confirm their proposed structures. The metabolites (2-6) were found to be identical with the synthesized compounds. These metabolites were orally administered to Triton WR-1339-induced hypertriglyceridemic rats, and the plasma levels of triglycerides were measured to estimate lipoprotein lipase activity. All the metabolites showed lower potency than NO-1886.
Goto
K
K
Laboratory of Drug Metabolism Research, Otsuka Pharmaceutical Factory, Inc., Tokushima, Japan.
Nakamura
S
S
Morioka
Y
Y
Kondo
M
M
Naito
S
S
Tsutsumi
K
K
D000818:Animals; D001549:Benzamides / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D001711:Biotransformation; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D006949:Hyperlipidemias / Q000097:blood / Q000139:chemically induced / Q000188:drug therapy; D008071:Lipoprotein Lipase / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009943:Organophosphorus Compounds / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D011092:Polyethylene Glycols; D051381:Rats; D017207:Rats, Sprague-Dawley; D014280:Triglycerides / Q000097:blood
D001549:Benzamides; D004791:Enzyme Inhibitors; D009943:Organophosphorus Compounds; D014280:Triglycerides; C082137:4-diethoxyphosphorylmethyl-N-(4-bromo-2-cyanophenyl)benzamide; D011092:Polyethylene Glycols; D008071:Lipoprotein Lipase; C016811:tyloxapol