作为角鲨烯合酶抑制剂的环戊二羧酸和环戊三羧酸：合成与评价
Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.
作者信息
Shen W, Garvey D S, Cohen J, Stein H, Rosenberg S H
机构信息
Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 1998 Apr 21;8(8):891-6. doi: 10.1016/s0960-894x(98)00143-7.
PMID:9871507
Abstract
Based on earlier lead squalene synthase inhibitor A-87049 (3) and zaragozic acids, a series of cyclopentanedi- and tricarboxylic acids were synthesized and evaluated against the enzyme. Some exhibited good potency and SAR revealed the importance of conformation and substitution pattern of these synthetic inhibitors.
摘要
基于早期的角鲨烯合酶抑制剂A-87049（3）和zaragozic酸，合成了一系列环戊二酸和三羧酸，并对该酶进行了评估。一些化合物表现出良好的活性，构效关系研究揭示了这些合成抑制剂的构象和取代模式的重要性。
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