| 摘要 |
PURPOSE:To provide a new N-hydroxyurea derivative capable of inhibiting lipoxygenase activity, useful for mitigating or curing the inflammatory diseases, allergies and cardiovascular diseases of mammals. CONSTITUTION:The objective compound of formula I [R1 is H, alkyl, alkenyl, alkylthioalkyl, cycloalkylamino, NR2R3 (R2 and R3 are each H, OH, alkyl, etc.), etc.; R4 is H, alkoxycarbonyl, alkanoyl or aroyl; A is alkylene or alkenylene; B is halogen, OH, alkoxy, hydroxyalkyl, alkyl, etc.; Ar is phenyl, naphthyl, pyridyl, quinolyl, thienyl, furyl, etc., each of which may bear substituent(s); m is 0-3; n is 0 or 1; p is 2 or 4; q is 1 or 2], e.g. N-[cis-3-(4- fluorophenyl)cyclobutyl]-N-hydroxyurea of formula II. The compound of the formula I can be obtained by reaction of trimethylsilyl isocyanate with a hydroxylamine of formula III produced from the corresponding ketone derivative for a cycloalkane. |
