Synthesis and biological evaluation of 5-[[3, 5-bis (1, 1-dimethylethyl)-4-hydroxyphenyl] methylene] oxazoles,-thiazoles, and-imidazoles: novel dual 5-lipoxygenase …

PC Unangst, DT Connor, WA Cetenko…

Index: Unangst, Paul C.; Connor, David T.; Cetenko, Wiaczeslaw A.; Sorenson, Roderick J.; Kostlan, Catherine R.; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 2 p. 322 - 328

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Citation Number: 163

Abstract

A variety of benzylideneoxazoles,-thiazoles, and-imidazoles derived from 2, 6-di-tert- butylphenol were prepared and evaluated as dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat basophilic leukemia (RBL-1) cells. The target compounds exhibit varying degrees of selectivity toward the two enzymes. Several compounds are orally active in the rat carageenan footpad edema (CFE) and mycobacterium footpad edema (MFE) ...