Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5

…, C Mathiesen, AS Kristensen, U Madsen

文献索引：Valgeirsson, Jon; Nielsen, Elsebet .; Peters, Dan; Mathiesen, Claus; Kristensen, Anders S.; Madsen, Ulf Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6948 - 6957

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被引用次数: 37

摘要

2-Arylureidobenzoic acids (AUBAs) have recently been presented as the first series of selective noncompetitive GluR5 antagonists. In this paper we have modified the acidic moiety of the AUBAs by introducing different acidic and neutral groups, and similarly, we have replaced the urea linker of the AUBAs with other structurally related linkers. Replacing the acid with neutral substituents led to inactive compounds in all instances, showing that ...