Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

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

ACS medicinal chemistry letters（2014）

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摘要

A series of nonsteroidal "dissociated" 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.

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关键词

Glucocorticoid mimetics,anti-inflammatory agents,azaindoles,drug-like properties,glucocorticoid-induced osteoporosis,nonsteroidal glucocorticoids

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