title: Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8 (IL-8) receptor antagonists.
abstract: A novel series of 3,5-diarylisoxazole and 3,5-diaryl-1,2,4-oxadiazole IL-8 inhibitors has been identified. These compounds exhibit activity in an IL-8 binding assay as well as in a functional assay of IL-8 induced elastase release from neutrophils. In addition, one of the compounds exhibits oral activity in a rat adjuvant arthritis model.
authors.affiliation: Johnson and Johnson Pharmaceutical Research and Development, LLC 1000 Route 202, Raritan, NJ 08869, USA. mwells@prdus.jnj.com
authors.forename: Michele A
authors.initials: MA
authors.lastname: Weidner-Wells
authors.forename: Todd C
authors.initials: TC
authors.lastname: Henninger
authors.forename: Stephanie A
authors.initials: SA
authors.lastname: Fraga-Spano
authors.forename: Christine M
authors.initials: CM
authors.lastname: Boggs
authors.forename: Michele
authors.initials: M
authors.lastname: Matheis
authors.forename: David M
authors.initials: DM
authors.lastname: Ritchie
authors.forename: Dennis C
authors.initials: DC
authors.lastname: Argentieri
authors.forename: Michael P
authors.initials: MP
authors.lastname: Wachter
authors.forename: Dennis J
authors.initials: DJ
authors.lastname: Hlasta
mesh_terms: D000284:Administration, Oral; D007555:Isoxazoles / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010069:Oxadiazoles / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D023062:Receptors, Interleukin-8A / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D007555:Isoxazoles; D010069:Oxadiazoles; D023062:Receptors, Interleukin-8A