Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: Pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2, 3-dihydro-6-( …

…, E Garver, LA Yodis, M Chabot-Fletcher…

Index: Adams, Jerry L.; Garigipati, Ravi S.; Sorenson, Margaret; Schmidt, Stanley J.; Brian, William R.; Newton, John F.; Tyrrell, Kathy A.; Garver, Eric; Yodis, Lee A.; Chabot-Fletcher, Marie; Tzimas, Maritsa; Webb, Edward F.; Breton, John J.; Griswold, Don E. Journal of Medicinal Chemistry, 1996 , vol. 39, # 26 p. 5035 - 5046

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Citation Number: 20

Abstract

A series of N-hydroxyurea derivatives have been prepared and examined as inhibitors of 5- lipoxygenase. Oral activity was established by examining the inhibition of LTB4 biosynthesis in an ex vivo assay in the mouse. The pharmacodynamic performance in the mouse of selected compounds was assessed using an ex vivo LTB4 assay and an adoptive peritoneal anaphylaxis assay at extended pretreat times. Compounds with an extended duration of ...