| 摘要 |
The present invention provides inhibitors of kynureninase having the formula <IMAGE> where X is CO or CHOH; RA and RB, independently of one another, are H, a halogen, a halovinyl group, or a small alkyl or haloalkyl group having one to three carbon atoms; A is a H or an acetyl group; R1 is H, NH2, NR6R7, NO2, halogen, CF3 or a small alkyl group having from one to three carbon atoms, wherein: R6 and R7, independently of one another, are H, a formyl group or a small alkyl group having from one to three carbon atoms with the exception that only one of R6 or R7 can be a formyl group; R2 is OH, H, halogen, CF3 or a small alkyl group having from one to three carbon atoms; and R3, R4 and R5, independently of one another, are H, halogen, CF3, NO2, NH2, or small alkyl group having from one to three carbon atoms, and with the proviso that when X=CO, neither RA nor RB can be CF3. In compounds of this formula in which X is CHOH, those having the ( alpha S, gamma S) configuration or the ( alpha R, gamma R) configuration when RA or RB is a hydrogen, are more potent inhibitors of kynureninase. Inhibitors of mammalian kynureninase are of particular use in therapy for certain neurological disorders. |
