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 …

…, TC Henninger, SA Fraga-Spano, CM Boggs…

Index: Weidner-Wells, Michele A.; Henninger, Todd C.; Fraga-Spano, Stephanie A.; Boggs, Christine M.; Matheis, Michele; Ritchie, David M.; Argentieri, Dennis C.; Wachter, Michael P.; Hlasta, Dennis J. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 16 p. 4307 - 4311

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Citation Number: 50

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.