TY - JOUR
T1 - Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor
AU - Obata, Rika
AU - Sunazuka, Toshiaki
AU - Otoguro, Kazuhiko
AU - Tomoda, Hiroshi
AU - Harigaya, Yoshihiro
AU - Omura, Satoshi
N1 - Funding Information:
We are grateful to Professor A. B. Smith, III and Dr. Itai for useful discussion and comments. This work was supported in part by a Grant-in-Aid for Scientific Research from the Ministry of Education, Science, Sports, and Culture of Japan.
PY - 2000/6/19
Y1 - 2000/6/19
N2 - Natural product acyl-CoA:cholesterol acyltrasferase (ACAT) inhibitor pyripyropene A was synthetically converted to acetylcholinesterase (AChE) inhibitor via heterolitic cleavage of the 2-pyrone ring, followed by γ-acylation/cyclization with several aroyl chlorides. The 4-pyridyl analogue selectively showed AChE inhibitory activity (IC50 = 7.9 μM) and no ACAT inhibitory activity IC50 = > 1000 μM. (C) 2000 Elsevier Science Ltd. All rights reserved.
AB - Natural product acyl-CoA:cholesterol acyltrasferase (ACAT) inhibitor pyripyropene A was synthetically converted to acetylcholinesterase (AChE) inhibitor via heterolitic cleavage of the 2-pyrone ring, followed by γ-acylation/cyclization with several aroyl chlorides. The 4-pyridyl analogue selectively showed AChE inhibitory activity (IC50 = 7.9 μM) and no ACAT inhibitory activity IC50 = > 1000 μM. (C) 2000 Elsevier Science Ltd. All rights reserved.
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U2 - 10.1016/S0960-894X(00)00218-3
DO - 10.1016/S0960-894X(00)00218-3
M3 - Article
C2 - 10890154
AN - SCOPUS:0034686427
SN - 0960-894X
VL - 10
SP - 1315
EP - 1316
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 12
ER -