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Summary
Novelty: Novel modified dipeptide compounds which may be useful for treating or preventing ulceration of tissue, especially the cornea, are disclosed. These compounds incorporate tryptophan or other fused or conjugated bicycloaromatic amino acid residues in a hydroxylamate-derivatized dipeptide matrix metalloprotease inhibitor.
Biology: The exemplified compound was assayed against crude or purified human skin fibroblast collagenase using the synthetic thiol ester substrate at pH 6.5 and gave a Ki value of 10nM. The prevention of corneal ulceration in the alkali-burned rabbit cornea was evaluated. The compound showed marked protection (100% over twenty-six days) of the cornea from perforation.
Chemistry: The syntheses of eighteen compounds are described in detail.
Structure: