Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities …

…, M Kanda, K Kurahashi, H Shirahase

Index: Takahashi, Kenji; Kasai, Masayasu; Ohta, Masaru; Shoji, Yoshimichi; Kunishiro, Kazuyoshi; Kanda, Mamoru; Kurahashi, Kazuyoshi; Shirahase, Hiroaki Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4823 - 4833

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Citation Number: 17

Abstract

A series of novel indoline derivatives with an ionizable moiety were synthesized to find a bioavailable acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor with antiperoxidative activity.[7-(2, 2-Dimethylpropanamido)-4, 6-dimethyl-1-octylindolin-5-yl] acetic acid hemisulfate (2, pactimibe sulfate) with low lipophilicity and high water solubility showed good oral absorption and inhibitory activity against foam cell formation in THP-1 cells ...