Title of article :
Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)
Author/Authors :
Rika Obata، نويسنده , , Toshiaki Sunazuka، نويسنده , , Hiroshi Tomoda، نويسنده , , Yoshihiro Harigaya، نويسنده , , Satoshi mura، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 1995
Abstract :
Modification and structure-activity relationships of ACAT inhibitor pyripyropene were examined. PR-109 (7g) showed the most potent (IC50 = 6 nM) inhibitory activity. PR-86 (2e) also had strong inhibitory activity (IC50 = 19 nM) and its in vivo activity improved 10 times better (ED50 = 10 mg/kg) than that of pyripyropene A.
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters