Title: Zileuton
CAS Registry Number: 111406-87-2
CAS Name: N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyurea
Additional Names: (±)-N-hydroxy-N-(1-benzo[b]thien-2-ylethyl)urea
Manufacturers' Codes: A-64077; Abbott 64077
Trademarks: Leutrol (Abbott); Zyflo (Abbott)
Molecular Formula: C11H12N2O2S
Molecular Weight: 236.29
Percent Composition: C 55.91%, H 5.12%, N 11.86%, O 13.54%, S 13.57%
Literature References: Inhibitor of 5-lipoxygenase, the initial enzyme in the biosynthesis of leukotrienes from arachidonic acid. Prepn: J. B. Summers, Jr. et al., EP 279263; eidem, US 4873259 (1988, 1989 both to Abbott). Chromatographic resolution of enantiomers: S. B. Thomas et al., J. Chromatogr. 623, 390 (1992). Inhibition of 5-lipoxygenase: G. W. Carter et al., J. Pharmacol. Exp. Ther. 256, 929 (1991). Pharmacokinetics: P. Rubin et al., Agents Actions Suppl. 35, 103 (1991). Clinical evaluation in rheumatoid arthritis: M. E. Weinblatt et al., J. Rheumatol. 19, 1537 (1992). Clinical trial in asthma: E. Israel et al., Ann. Intern. Med. 119, 1059 (1993). Reviews: R. L. Bell et al., Int. J. Immunopharmacol. 14, 505-510 (1992); K. McGill, W. W. Busse, Lancet 348, 519-524 (1996).
Properties: Crystals, mp 157-158°.
Melting point: mp 157-158°
Therap-Cat: Antiasthmatic.
Keywords: Antiasthmatic (Nonbronchodilator); 5-Lipoxygenase Inhibitor. |