oxocarboxylic acids and estersoxocarboxylic acids and esters (benzene compounds) Q 0460
-0824-Phenyl-4-oxo-butanoic Acid Derivatives Inhibitors of Kynurenine 3-Hydroxylase.-A new class of inhibitors, derived from a structure-activity relationship study of the benzoylalanine side chain of a potent previously synthesized KYN-3-OHase inhibitor, is presented. The enantiomers (III) and (VI) show robust enzymatic inhibition, selectivity towards other kynurenine pathway enzymes and specificity against other monooxygenases. Both enantiomers of (VI) are obtained via diastereomeric salt resolution using ephedrine. -(GIORDANI, A.; PEVARELLO, P.; CINI, M.; BORMETTI, R.; GRECO, F.; TOMA, S.; SPECIALE, C.; VARASI, M.; Bioorg. Med. Chem.
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