Inhibitor development for 4-hydroxyphenylpyruvate dioxygenase, employing tyrosinemia 1 as a model for human diseases mediated by 2-oxoacid utilizing dioxygenases
申请人:Hanauske-Abel M. Hartmut
公开号:US20050288187A1
公开(公告)日:2005-12-29
The present invention is directed to a method of inhibiting 4-hydroxyphenylpyruvate dioxygenase in a living system by administering to the living system an effective amount of a compound of formulas I or II or III or derivatives thereof as follows: R
1
, R
2
, R
3
, and R
4
each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms under conditions effective to inhibit 4-hydroxyphenylpyruvate dioxygenase in the living system. These compounds are also useful in carrying out a method of treating a patient and a method of regulating plant growth.
本发明涉及通过向生物体内投与式I或II或III或其衍生物的有效量来抑制生物体内4-羟基苯丙酮酸双氧酶的方法,其中:R1,R2,R3和R4分别表示氢,含1至约8个碳原子的烷基,烯基或烷氧基,含约5至12个碳原子的芳基,芳基烷基或环烷基,含多达8个碳原子的羧基烷氧基或氨基甲酰基,或含有10至约30个碳原子的肽或类肽基团,在有效条件下抑制生物体内的4-羟基苯丙酮酸双氧酶。这些化合物还可用于进行治疗患者的方法和调节植物生长的方法。