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. The synthesis...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (3), p.633-637
Hauptverfasser:	Sawada, Masae, Washizuka, Ken-ichi, Okumura, Hiroyuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzylamines - chemical synthesis Benzylamines - pharmacology Biological and medical sciences Cholesterol - blood Dogs Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins Humans In Vitro Techniques Medical sciences Microsomes, Liver - enzymology Oxygenases - antagonists & inhibitors Pharmacology. Drug treatments Rats Squalene Monooxygenase Structure-Activity Relationship Triglycerides - blood Tumor Cells, Cultured
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Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.11.072