Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid

MN Greco, WE Hageman, ET Powell…

Index: Greco; Hageman; Powell; Tighe; Persico Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3180 - 3183

Full Text: HTML

Citation Number: 19

Abstract

A novel series of N-[(2-benzothiazolylthio) alkyl]-N'-hydroxyurea derivatives (9-25) was synthesized and evaluated for biological activity as inhibitors of 5-lipoxygenase both in vivo (mouse zymosan peritonitis assay) and in vitro (Ca2+ ionophore-stimulated human peripheral blood leukocyte model). The compounds of this series were based on the corresponding hydroxamic acid derivatives (1, 3, 4, and 5) which were moderately active ...