| 摘要 |
PURPOSE: Pyrrol-1-yl benzene sulfonyl amino acids and a preparation method thereof are provided, which amino acids are matrix metalloproteinase inhibitors, so that the amino acids are useful for prevention and treatment of disease associated with the matrix metalloproteinase including angiogenesis related cancer, periodontal disease and arthritis. CONSTITUTION: The pyrrol-1-yl benzene sulfonyl amino acids represented by formula (1), enantiomers thereof, pharmaceutically acceptable salts thereof, or solvates thereof are provided, wherein Y is OH or NHOH; X is hydrogen, lower alkyl, higher alkyl, double bond containing higher alkyl, aryl, heteroaryl, halogen, O-lower alkyl, O-heteroaryl, alkyl-amine derivatives, or alkyl-carboxylic acid derivatives; and R is hydrogen, side chains of all natural amino acids or derivatives thereof, lower alkyl, aryl, heteroaryl, 4- to 8-membered ring compound containing lower alkyl, 4- to 8-membered hetero ring compounds, or 4- to 8-membered hetero ring containing lower alkyl, provided that X and R form a ring to prepare 5- to 8-membered compounds which preferably comprises proline and hydroxyproline derivatives, and N, O or S substituted hetero ring compound and derivatives thereof in the 5- to 8-membered ring.
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