Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738.
The synthesis and biological properties of a novel squalene epoxidase inhibitor, FR194738, are described. This compound displayed potent in vitro inhibitory activities against squalene epoxidase and cholesterol synthesis, and lowered plasma cholesterol and triglyceride levels in dogs.
Sawada
Masae
M
Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co Ltd, 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. masae_sawada@po.fujisawa.co.jp
Washizuka
Ken ichi
Ki
Okumura
Hiroyuki
H
D000818:Animals; D001596:Benzylamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood*; D004285:Dogs; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008862:Microsomes, Liver / Q000201:enzymology*; D010105:Oxygenases / Q000037:antagonists & inhibitors*; D051381:Rats; D050603:Squalene Monooxygenase; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood*; D014407:Tumor Cells, Cultured
D001596:Benzylamines; D004791:Enzyme Inhibitors; C443179:FR 194738; D014280:Triglycerides; D002784:Cholesterol; D010105:Oxygenases; D050603:Squalene Monooxygenase