Optimization of Drug-Like Properties of Nonsteroidal Glucocorticoid Mimetics and Identification of a Clinical Candidate
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- 作者：Christian Harcken ; Doris Riether ; Pingrong Liu ; Hossein Razavi ; Usha Patel ; Thomas Lee ; Todd Bosanac ; Yancey Ward ; Mark Ralph ; Zhidong Chen ; Donald Souza ; Richard M. Nelson ; Alison Kukulka ; Tazmeen N. Fadra-Khan ; Ljiljana Zuvela-Jelaska ; Mita Patel ; David S. Thomson ; Gerald H. Nabozny
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2014
- 出版时间：December 11, 2014
- 年：2014
- 卷：5
- 期：12
- 页码：1318-1323
- 全文大小：254K
- ISSN：1948-5875
文摘
A series of nonsteroidal 鈥渄issociated鈥?glucocorticoid receptor agonists was optimized for drug-like properties such as cytochrome P450 inhibition, metabolic stability, aqueous solubility, and hERG ion channel inhibition. This effort culminated in the identification of the clinical candidate compound (R)-39.