| abstract |
Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: <IMAGE> wherein: Y represents hydrogen or fluorine; Z represents -CH2NR1R2, where R1 and R2 are as defined below, or -COR3 where R3 is as defined below; Ra represents hydrogen or R4, where R4 is as defined below; R1 represents hydrogen, C1-C6 alkyl or phenyl-(C1-C4 alkyl); R2 represents hydrogen, C1-C6 alkyl, phenyl-(C1-C4 alkyl) or, when Ra is hydrogen, R4, where R4 is as defined below; R3 represents hydroxy, or when Ra is hydrogen, C1-C8 alkoxy, -NR5R6, where R5 and R6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid; each R4, independently, represents C2-C5 alkylcarbonyl, phenylcarbonyl, phenyl-(C1-C4 alkyl)-carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid; R5 and R6, independently, represent hydrogen or C1-C4 alkyl; and P represents 1 or 2. |