TY - JOUR
T1 - Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA
T2 - Cholesterol O-acyltransferase (ACAT)
AU - Obata, Rika
AU - Sunazuka, Toshiaki
AU - Tomoda, Hiroshi
AU - Harigaya, Yoshihiro
AU - Omura, Satoshi
PY - 1995/11/16
Y1 - 1995/11/16
N2 - 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.
AB - 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.
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U2 - 10.1016/0960-894X(95)00451-X
DO - 10.1016/0960-894X(95)00451-X
M3 - Article
AN - SCOPUS:0028829655
SN - 0960-894X
VL - 5
SP - 2683
EP - 2688
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 22
ER -