Synthesis and structureactivity relationship of pyripyropene A derivatives as potent and selective acyl-CoA: cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 1

M Ohtawa, H Yamazaki, S Ohte, D Matsuda… - Bioorganic & medicinal …, 2013 - Elsevier
… –activity relationship studies were carried out using derivatives based on pyripyropene A
(PPPA… We have successfully developed novel PPPA derivatives with a 7-O-substituted benzoyl …

Synthesis and structureactivity relationship of pyripyropene A derivatives as potent and selective acyl-CoA: cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 3

M Ohtawa, H Yamazaki, S Ohte, D Matsuda… - Bioorganic & medicinal …, 2013 - Elsevier
… In an effort to develop potent and selective inhibitors toward ACAT2, structureactivity
relationship studies were carried out using derivatives based on pyripyropene A (PPPA, 1). In …

Chemical Modification and Structure-activity Relationships of Pyripyropenes 2. 1, 11-Cyclic Analogs

R Obata, T Sunazuka, Y Kato, H Tomoda… - The Journal of …, 1996 - jstage.jst.go.jp
32 C28H33O7N 496.2346(M+ H) 35 C29H37O7N 512.2650 (M+ H) 17 C30H39O7N
526.2808(M+ H) 21 C27H33O8N 500.2310 (M+ H) 83 C32H35O7N 546.2500(M+ H) 85 …

Chemical Modification and Structure-activity Relationships of Pyripyropenes 3. Synthetic Conversion of Pyridine-pyrone Moiety

R Obata, T Sunazuka, Z Tian, H Tomoda… - The Journal of …, 1997 - jstage.jst.go.jp
Structure-activity relationships of the pyridine-pyrone moiety in pyripyropene A(1), a potent
acyl-CoA : cholesterol acyltransferase (ACAT)inhibitor of fungal origin, were studied. Several …

Synthesis and structureactivity relationship of pyripyropene A derivatives as potent and selective acyl-CoA: cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 2

M Ohtawa, H Yamazaki, D Matsuda, T Ohshiro… - Bioorganic & medicinal …, 2013 - Elsevier
Synthesis and structureactivity relationships of 7-O-p-cyanobenzoyl pyripyropene A
derivatives with modification at C1 and 11 are described. Regioselective mono-deprotection …

Chemical Modification and Structure-activity Relationships of Pyripyropenes 1. Modification at the Four Hydroxyl Groups

R Obata, T Sunazuka, Z Li, Z Tian, Y Harigaya… - The journal of …, 1996 - jstage.jst.go.jp
… of pyripyropenes have … )activity in vitro and to lower cholesterol absorption in vivo in a
cholesterol-fed hamster. 7-0-«-Valeryl derivative (8c) improved the in vitro ACATinhibitory activity (…

Synthesis of pyripyropene derivatives and their pest-control efficacy

K Goto, R Horikoshi, S Nakamura, M Mitomi… - Journal of Pesticide …, 2019 - jstage.jst.go.jp
… , 13k showed moderate tickicidal activity through contact application. The structure and activity
relationship (SAR) appeared to be different from that for insecticidal activity. Therefore, we …

Design and Synthesis of A‐Ring Simplified Pyripyropene A Analogues as Potent and Selective Synthetic SOAT2 Inhibitors

M Ohtawa, S Arima, N Ichida, T Terayama… - …, 2018 - Wiley Online Library
synthesized based on total synthesis, and the results of structureactivity relationship studies
of pyripyropene A… Among the analogues, two A-ring simplified pyripyropene A analogues …

Synthesis and insecticidal efficacy of pyripyropene derivatives. Part II—Invention of afidopyropen

K Goto, R Horikoshi, M Mitomi, K Oyama… - The Journal of …, 2019 - nature.com
activity [16]. We investigated the structureactivity relationship (SAR) of these PP derivatives
… aphids, superior to that of derivative 1, taking systemic activity into consideration. In the …

Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)

R Obata, T Sunazuka, H Tomoda, Y Harigaya… - Bioorganic & Medicinal …, 1995 - Elsevier
activity. Based on the structure-activity relationships described above, we propose here the
binding model of the most potent derivative PR-109 (Tg) to ACAT (Fig. 1). The phenyl group …