Document Report Card

ID: ALA1125893

Journal: J Med Chem

Title: Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.

Authors: Flynn DL, Belliotti TR, Boctor AM, Connor DT, Kostlan CR, Nies DE, Ortwine DF, Schrier DJ, Sircar JC.

Abstract: A series of styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles were prepared and found to be dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat basophilic leukemia cells. Compounds from this series also were found to inhibit the in vivo production of LTB4 when dosed orally in rats. Among these compounds, di-tert-butylphenols 19 and 33 exhibit oral activity in various models of inflammation and, most importantly, are devoid of ulcerogenic potential.

CiteXplore: 1847426

DOI: 10.1021/jm00106a006