期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 15, 页码 3268-3273出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.06.010
关键词
Acylurea; Imide; Isostere; Glucocorticoid receptor; Non-steroidal glucocorticoid receptor agonists
Acylureas and acyclic imides are found to be excellent isosteres for 2-acylamino-1,3,4-thiadiazole in the azaxanthene-based series of glucocorticoid receptor (GR) agonists. The results reported herein show that primary acylureas maintain high affinity and selectivity for GR while providing improved CYP450 inhibition and pharmacokinetic profile over 2-acylamino-1,3,4-thiadiazoles. General methods for synthesis of a variety of acylureas and acyclic imides from a carboxylic acid were utilized and are described. (C) 2014 Elsevier Ltd. All rights reserved.
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