2. Academic Validation
  3. Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors

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

  • J Med Chem. 1991 Feb;34(2):518-25. doi: 10.1021/jm00106a006.
D L Flynn 1,  T R Belliotti,  A M Boctor,  D T Connor,  C R Kostlan,  D E Nies,  D F Ortwine,  D J Schrier,  J C Sircar
Affiliations

Affiliation

  • 1 Department of Chemistry, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.
PMID: 1847426 DOI: 10.1021/jm00106a006
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.

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