新型强效口服活性酰基辅酶A：胆固醇O-酰基转移酶（ACAT）抑制剂FR186054的合成、X射线晶体结构及生物活性，该抑制剂含有吡唑环。

Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) bearing a pyrazole ring.

作者信息

Tanaka A, Terasawa T, Hagihara H, Kinoshita T, Sakuma Y, Ishibe N, Sawada M, Takasugi H, Tanaka H

机构信息

Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd., Osaka, Japan.

出版信息

Bioorg Med Chem Lett. 1998 Jan 6;8(1):81-6. doi: 10.1016/s0960-894x(97)10191-3.

DOI:10.1016/s0960-894x(97)10191-3

Abstract

The synthesis, single crystal X-ray structural analysis, and biological activity of FR186054 (2c), a new, potent, orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT), containing a pyrazole ring are described. This compound displayed excellent in vitro efficacy, irrespective of dosing method, indicating superior characteristics compared to other ACAT inhibitors.

摘要

本文描述了新型强效口服有效酰基辅酶A：胆固醇O-酰基转移酶（ACAT）抑制剂FR186054（2c）的合成、单晶X射线结构分析及生物活性，该抑制剂含有一个吡唑环。无论给药方式如何，该化合物均表现出优异的体外药效，表明其与其他ACAT抑制剂相比具有更优越的特性。

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