| Literature DB >> 25455491 |
Hongfu Lu1, Ting Yang1, Zhongmiao Xu1, Paul B Wren1, Yueting Zhang1, Xin Cai1, Metul Patel2, Kelly Dong1, Qing Zhang1, Wei Zhang1, Xiaoming Guan1, Jianing Xiang1, John D Elliott1, Xichen Lin1, Feng Ren3.
Abstract
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.Entities:
Keywords: 2-Aminopyrimidin-4(1H)-one; Bioisostere; CXCR2 antagonists; Urea
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Year: 2014 PMID： 25455491 DOI： 10.1016/j.bmcl.2014.10.003
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823