947536-15-4Relevant academic research and scientific papers
Discovery of potent and specific CXCR3 antagonists
Chen, Xiaoqi,Mihalic, Jeff,Deignan, Jeff,Gustin, Darin J.,Duquette, Jason,Du, Xiaohui,Chan, Johann,Fu, Zice,Johnson, Michael,Li, An-Rong,Henne, Kirk,Sullivan, Tim,Lemon, Bryan,Ma, Ji,Miao, Shichang,Tonn, George,Collins, Tassie,Medina, Julio C.
, p. 357 - 362 (2012/03/11)
The optimization of a series of 8-aza-quinazolinone analogs for antagonist activity against the CXCR3 receptor is reported. Compounds were optimized to avoid the formation of active metabolites and time-dependent-inhibitors of CYP3A4. In addition, antagon
Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists
Storelli, Stefania,Verzijl, Dennis,Al-Badie, Jawad,Elders, Niels,Bosch, Leontien,Timmerman, Henk,Smit, Martine J.,De Esch, Iwan J. P.,Leurs, Rob
, p. 281 - 291 (2008/02/10)
CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-pheny
