473720-84-2Relevant academic research and scientific papers
Construction of N-Boc-2-Alkylaminoquinazolin-4(3H)-Ones via a Three-Component, One-Pot Protocol Mediated by Copper(II) Chloride that Spares Enantiomeric Purity
Li, Xiaoyu,Golden, Jennifer E.
supporting information, p. 1638 - 1645 (2021/02/09)
Chiral 2-alkylquinazolinones are key synthetic intermediates, but their preparation in high optical purity is challenging. Thus, a multicomponent procedure integrating anthranilic acids, N-Boc-amino acids, and amines in the presence of methanesulfonyl chl
Optimization of a series of quinazolinone-derived antagonists of CXCR3
Liu, Jiwen,Fu, Zice,Li, An-Rong,Johnson, Michael,Zhu, Liusheng,Marcus, Andrew,Danao, Jay,Sullivan, Tim,Tonn, George,Collins, Tassie,Medina, Julio
scheme or table, p. 5114 - 5118 (2010/03/31)
The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoi
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3
Johnson, Michael,Li, An-Rong,Liu, Jiwen,Fu, Zice,Zhu, Liusheng,Miao, Shichang,Wang, Xuemei,Xu, Qingge,Huang, Alan,Marcus, Andrew,Xu, Feng,Ebsworth, Karen,Sablan, Emmanuel,Danao, Jay,Kumer, Jeff,Dairaghi, Dan,Lawrence, Chris,Sullivan, Tim,Tonn, George,Schall, Thomas,Collins, Tassie,Medina, Julio
, p. 3339 - 3343 (2008/02/11)
A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a 125I-IP10 displacement assay and in in vitro cell migration assays to IP10, IT
CXCR3 antagonists
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, (2008/06/13)
Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
