Bioavailable Acyl-CoA. Cholesterol Acyltransferase Inhibitor with Anti-peroxidative Activity. Synthesis and Biological Activity of Novel Indolinyl Amide and Urea Derivatives.

Inhibitory Effect of Acyl-CoA: Cholesterol Acyltransferase Inhibitor-Low Density Lipoprotein Complex on Experimental Atherosclerosis.

“…KV-2920 is a potent antioxidant. 13) Antioxidants are believed to be beneficial in atherosclerosis because they prevent oxidative modification of native LDL and so inhibit the foam cell formation of macrophages. Indeed, it has been reported that antioxidants could play a potential role in the prevention of atherosclerosis by inhibiting incorporation of oxidized LDL into macrophages.…”

“…13) Since it is necessary, however, that any drug to be incorporated into LDL be highly lipophilic, 14) this appears to make it appropriate for use in a drug-LDL complex to treat atherosclerosis.…”

Novel Acyl-CoA: Cholesterol Acyltransferase Inhibitor: Indoline-Based Sulfamide Derivatives with Low Lipophilicity and Protein Binding Ratio

“…Compound 2 was synthesized from 1-acetyl-4,6-dimethylindoline according to the method previously reported 11) and then nitrated to give compound 3 with a nitro group at the 5-position. To prepare 1a-f, h-k, compound 3 was hydrolyzed to give compound 4 with no substituents at the 1-position, and then various chains, e.g.…”

“…3,5-Dimethylphenylhydrazine (10) was converted to 2,4,6-trimethylindole (11) by Fisher indole synthesis. Compound 11 was reduced by NaBH 3 CN and acetylated at the 1-position to give compound 12.…”

“…Compound 27 (Pactimibe) with a carboxymethyl moiety, and compounds 28 (KY-455) and 29 with no substituents at the 5-position were synthesized according to the methods previously reported. 7,11) …”