Orally active inhibitors of stromelysin-1 (MMP-3)

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 7, 1996, Pages 803-806

  Chapman, Kevin T ^a   Durette, Philippe L ^a   Caldwell, Charles G ^a   Sperow, Kelly M ^a   Niedzwiecki, Lisa M ^a   Harrison, Richard K ^a,b   Saphos, Cheryl ^a   Christen, Amy J ^a   Olszewski, Julie M ^a   Moore, Vernon L ^a   MacCoss, Malcolm ^a   Hagmann, William K ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b SANOFI   (France)

Author keywords

[No Author keywords available]

Indexed keywords

DIPEPTIDE; ISOENZYME; N (1 PHENYLAMINOCARBONYL 3 METHYLBUTYL) 2 (2 CARBOXYPROPYL) 4 (4 PROPYLPHENYL)BUTYRAMIDE; STROMELYSIN; STROMELYSIN INHIBITOR; TRANSFERRIN; UNCLASSIFIED DRUG;

ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG SYNTHESIS; ENZYME INHIBITION; LUNG; MOUSE; NONHUMAN; ORAL DRUG ADMINISTRATION; STRUCTURE ACTIVITY RELATION;

ANIMALIA;

EID: 0029876143     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00109-6     Document Type: Article

References (13)

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8. Dosing vehicles: (iv) 2% DMSO, 2% Cremaphore, 96% PBS; (po) 2% DMSO, 2% Cremaphore, 96% aq. solution of 0.25% carboxymethylcellulose.
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10. 3, 0.05% Brij.
11. % degradation = TCA soluble counts/ total counts % inhibition = 1 - (% degradation w/ inhibitor solution) - (% degradation w/ MMP-3 buffer/ (% degradation w/o MMP-3 added) - (% degradation w/ MMP-3 buffer)
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