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Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists. 2008

Jean-Pierre Bongartz, and Mieke Buntinx, and Erwin Coesemans, and Bart Hermans, and Guy Van Lommen, and Jean Van Wauwe
Johnson & Johnson PRD, RED EU, Turnhoutseweg 30, B-2340 Beerse, Belgium. jbongart@its.inj.com

The synthesis and evaluation of benzetimide derivatives showing potent CXCR3 antagonism are described. Optimization of the screening hits led to the identification of more potent CXCR3 antagonists devoid of anti-cholinergic activity and identification of the key pharmacophore moieties of the series.

UI MeSH Term Description Entries
D003909 Dexetimide A muscarinic antagonist that has been used to treat neuroleptic-induced parkinsonism. Benzetimide is the (-)-enantimorph of dexetimide. Benzetimide,Dexbenzetimide,Dexbenzetimid,R-16470,Spasmentral,Tremblex,dextro-Benzetimide,R 16470,R16470,dextro Benzetimide
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D054367 Receptors, CXCR3 CXCR receptors that are expressed on the surface of a number of cell types, including T-LYMPHOCYTES; NK CELLS; DENDRITIC CELLS; and a subset of B-LYMPHOCYTES. The receptors are activated by CHEMOKINE CXCL9; CHEMOKINE CXCL10; and CHEMOKINE CXCL11. Antigens, CD183,CD183 Antigens,CXC Chemokine Receptor 3,CXCR3 Receptors,CMKBR3 Chemokine Receptors,CXC Chemokine Receptors 3,CXCR3 Receptor,Chemokine (C-C Motif) Receptor 3,Chemokine Receptors, CMKBR3,Receptor, CXCR3,Receptors, CMKBR3 Chemokine

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