Inhibitors of kynureninase

Details Inhibitors of kynureninase Inhibitors of kynureninase

1991-04-18

1993-10-19

Dees, Jose G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

560 39, C07C22936, A61K 31195

Patent

active

052547256

ABSTRACT:
The present invention provides inhibitors of kynureninase having the formula ##STR1## where R.sub.a and R.sub.b, independently of one another are H, a halogen, CF.sub.3 or a small alkyl group having one to three carbon atoms; R.sub.1 is NH.sub.2, NR.sub.6 R.sub.7, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms, wherein R.sub.6 and R.sub.7, 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 R.sub.6 or R.sub.7 can be a formyl group; R.sub.2 is OH, H, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms; and R.sub.3, R.sub.4 and R.sub.5, independently of one another, are H, halogen, CF.sub.3 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 R.sub.A or R.sub.B is a halogen are more potent inhibitors of kynureninase. Inhibitors of mammalian kynureninase are of particular use in therapy for certain neurological disorders.

REFERENCES:
*Phillips and Dua J. Amer. Chem. Soc. 113:7385-7388 (1991).
Soda, K. and Tanizawa, K. (1979) Advances in Enzymology 49:1-40.
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Hayaishi, O. (1955) in A Symposium on Amino Acid Metabolism, W. D. McElroy & H. B. Glass eds. Johns Hopkins Press Baltimore, pp. 914-929.

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