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Volumn 45, Issue 26, 2002, Pages 5628-5639

NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability

Author keywords

[No Author keywords available]

Indexed keywords

1 NAPHTHYLHYDROXAMATE; HYDROXAMIC ACID DERIVATIVE; MATRIX METALLOPROTEINASE INHIBITOR; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; UNCLASSIFIED DRUG;

EID: 0037137618     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm020160g     Document Type: Article
Times cited : (72)

References (19)
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    • note
    • It should be noted that the inhibitory activity observed in the blood during the PK studies cannot formally be attributed to the parent compound, as an active metabolite could also contribute to enzymatic inhibition. However, the most likely metabolite would be the corresponding carboxylic acid, which would be predicted to have little or no activity (See ref 2). In fact, the carboxylic analogue of the initial inhibitor 3 exhibited a more than 100-fold loss in potency compared to the hydroxamate-containing parent (ref 12).
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