The invention relates to new basic amino acid derivatives of general formula
I and the preparation and use thereof in treatment of pain. The compounds have
histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating
activities.
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wherein:
- A is -hydrogen, —(C1-C8)alkyl or —(C1-C8)alkyl
substituted by hydroxy;
- B is —(C1-C6)alkylguanidino, —(C1-C6)alkyl(4-imidazo-lyl),
—(C1-C6)alkylamino, p-aminophenylalkyl(C1-C6)—,
p-guanidinophenylalkyl(C1-C6)— or 4-pyridinylalkyl(C1-C6)—;
- R1, R2 and R3 are, independent of one
another, -hydrogen, -arylcarbonylamino, —(C1-C6)alkoylamino,
—(C1-C6)alkylamino, —(C1-C6)alkyloxy,
—(C1-C6)alkylaminocarbonyl, -carboxy, —OH, -benzoyl,
-p-halogenobenzoyl, -methyl, —S-(2,4-dinitrophenyl), —S-(3-nitro-2-pyridinesulfenyl),
-sulfonyl, -trifluoromethyl, —(C1-C6)alkylaminocarbonylamino,
-halo or -amino;
- R4 and R5 are, independent of one another, -hydrogen,
—(C1-C6)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino,
—(C1-C6)alkoylamino, —(C1-C6)alkylamino,
-halo or —OH.
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