title: Discovery of a novel series of CXCR3 antagonists.
abstract: The discovery of a novel series of CXCR3 antagonists is described. Starting from an HTS positive, iterative optimization gave potent compounds (IC(50) 15 nM in a chemotaxis assay). The strategy employed to improve the metabolic stability of these derivatives is described.
authors.affiliation: Merck Serono SA, Geneva, Switzerland. stefano.crosignani@merckserono.net
authors.forename: Stefano
authors.initials: S
authors.lastname: Crosignani
authors.forename: Marc
authors.initials: M
authors.lastname: Missotten
authors.forename: Christophe
authors.initials: C
authors.lastname: Cleva
authors.forename: Ruggero
authors.initials: R
authors.lastname: Dondi
authors.forename: Yann
authors.initials: Y
authors.lastname: Ratinaud
authors.forename: Yves
authors.initials: Y
authors.lastname: Humbert
authors.forename: Ashis Baran
authors.initials: AB
authors.lastname: Mandal
authors.forename: Agnès
authors.initials: A
authors.lastname: Bombrun
authors.forename: Christine
authors.initials: C
authors.lastname: Power
authors.forename: André
authors.initials: A
authors.lastname: Chollet
authors.forename: Amanda
authors.initials: A
authors.lastname: Proudfoot
mesh_terms: D000818:Animals; D002460:Cell Line; D002633:Chemotaxis / Q000187:drug effects*; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008861:Microsomes; D051381:Rats; D054367:Receptors, CXCR3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000502:physiology
chemical_list: D054367:Receptors, CXCR3