1. Academic Validation
  2. Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT)

Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT)

  • Bioorg Med Chem Lett. 1999 Jul 19;9(14):2039-42. doi: 10.1016/s0960-894x(99)00330-3.
N Matsuyama 1 T Kosaka M Fukuhara Y Soda K Mizuno
Affiliations

Affiliation

  • 1 R & D Facilities, Azwell Inc., Osaka, Japan.
Abstract

A series of polyunsaturated fatty acid anilides were synthesized and evaluated as ACAT inhibitors. Compound 24 had potent inhibitory activity against microsomal ACAT derived from U937, HepG2 and Caco-2 cell lines. Therefore, it might be expected to act as an antiarteriosclerotic and hypocholesterolemic agent. Interestingly, the ACAT inhibitory potency of 24 varied significantly depending on the source of the enzyme.

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