title: Evaluation of WO2012080456 and WO2012080457; Boheringer Ingleheim's first CXCR2 antagonists.
abstract: Two applications claim CXCR2 receptor antagonists respectively incorporating arylcarbonyl and arylsulfonyl substituted 2-hydroxyaniline scaffolds. The first application claims both N-aryl,N'-aryl urea and squaramide derivatives, the second focuses on squaramide derivatives. Several examples of the latter scaffold with nanomolar affinity are provided and indicate an alternative modification of the squaramide scaffold that has been explored extensively by other groups.
authors: Norman Consulting, 18 Pink Lane, Burnham, Bucks SL1 8JW, UK. peter.norman2@btinternet.com
authors: Peter
authors: P
authors: Norman
mesh_terms: D000627:Aminophenols / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002633:Chemotaxis / Q000187:drug effects; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D016209:Interleukin-8 / Q000037:antagonists & inhibitors / Q000494:pharmacology; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000627:Aminophenols; D016209:Interleukin-8; D023063:Receptors, Interleukin-8B; D013449:Sulfonamides