作为纤溶酶原激活物抑制剂-1抑制剂的恶二唑烷二酮的设计与合成
Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.
作者信息
Gopalsamy Ariamala, Kincaid Scott L, Ellingboe John W, Groeling Thomas M, Antrilli Thomas M, Krishnamurthy Girija, Aulabaugh Ann, Friedrichs Gregory S, Crandall David L
机构信息
Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jul 5;14(13):3477-80. doi: 10.1016/j.bmcl.2004.04.058.
PMID:15177456
Abstract
A novel series of PAI-1 inhibitors containing an oxadiazolidinedione moiety were identified by high through-put screening. Optimization of substituents by parallel synthesis and the iterative design toward understanding structure-activity relationship to improve potency are described.
摘要
通过高通量筛选鉴定出了一系列含有恶二唑二酮部分的新型PAI-1抑制剂。描述了通过平行合成对取代基进行优化以及为理解构效关系以提高效力而进行的迭代设计。
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