| 摘要 |
The present invention provides inhibitors of kynureninase having the formula <IMAGE> where Ra and Rb, independently of one another are H, a halogen, CF3 or a small alkyl group having one to three carbon atoms; R1 is NH2, NR6R7, 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 or small alkyl group having from one to three carbon atoms. In particular, compounds of formula I having the ( alpha S, gamma S) configuration or ( alpha R, gamma R) configuration when RA or RB is a halogen are more potent inhibitors of kynureninase. Inhibitors of mammalian kynureninase are of particular use in therapy for certain neurological disorders.
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