期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 23, 页码 5493-5496出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.10.003
关键词
2-Aminopyrimidin-4(1H)-one; Bioisostere; Urea; CXCR2 antagonists
2-Aminopyrimidin-4(1H)-one was proposed as the novel bioisostere of urea. Bioisosteric replacement of the reported urea series of the CXCR2 antagonists with 2-aminopyrimidin-4(1H)-ones led to the discovery of the novel and potent CXCR2 antagonist 3e. 2-Aminopyrimidin-4(1H)-one derivative 3e demonstrated a good developability profile (reasonable solubility and high permeability) and superior chemical stability especially in simulated gastric fluid (SGF) compared with ureas. (C) 2014 Elsevier Ltd. All rights reserved.
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