Zileuton is the only FDA-approved 5-lipoxygenase (5-LOX) inhibitor for asthma treatment, but it produces hepatotoxicity associated with the benzothiophene fragment. Using the concept of organometallic derivatization pioneered by Jaouen and Brocard, we synthesized five new organometallic Zileuton derivatives, maintaining the urea fragment and incorporating ferrocenyl and ruthenocenyl moiety (