Nonsteroidal Dissociated Glucocorticoid Agonists Containing Azaindoles as Steroid A-Ring Mimetics
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- 作者：Doris Riether ; Christian Harcken ; Hossein Razavi ; Daniel Kuzmich ; Thomas Gilmore ; Jrg Bentzien ; Edward J. Pack ; Jr. ; Donald Souza ; Richard M. Nelson ; Alison Kukulka ; Tazmeen N. Fadra ; Ljiljana Zuvela-
- 刊名：Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：September 23, 2010
- 年：2010
- 卷：53
- 期：18
- 页码：6681-6698
- 全文大小：1273K
- 年卷期：v.53,no.18(September 23, 2010)
- ISSN：1520-4804
文摘
Syntheses and structure−activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene transrepression and transactivation. Collagen induced arthritis studies in mouse have demonstrated that in vitro dissociated compounds (R)-16 and (R)-37 have steroid-like anti-inflammatory properties with improved metabolic side effect profiles, such as a reduced increase in body fat and serum insulin levels, compared to steroids.