The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 19, 1999, Pages 2887-2892

  Martin, Fionna M ^a   Beckett, R Paul ^a   Bellamy, Claire L ^a   Courtney, Paul F ^a   Davies, Stephen J ^a   Drummond, Alan H ^a   Dodd, Rory ^a   Pratt, Lisa M ^a   Patel, Sanjay R ^a   Ricketts, Michelle L ^a   Todd, Richard S ^a   Tuffnell, Andrew R ^a   Ward, John W S ^a   Whittaker, Mark ^a  

^a British Biotech Pharmaceuticals Ltd   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

COLLAGENASE INHIBITOR; MATRIX METALLOPROTEINASE INHIBITOR; SULFONAMIDE;

ANIMAL EXPERIMENT; ARTICLE; BIOASSAY; CHEMICAL MODIFICATION; CHEMICAL REACTION; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; NONHUMAN; RAT; STEREOCHEMISTRY;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; HYDROGEN BONDING; HYDROXAMIC ACIDS; MATRIX METALLOPROTEINASES; MOLECULAR STRUCTURE; PROTEASE INHIBITORS; RATS; SULFONAMIDES;

ANIMALIA;

EID: 0033523714     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00494-1     Document Type: Article

References (20)

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19. 9. a) The following literature procedure was adapted to determine the potency of compounds against recombinant MMP enzymes. Knight, C. G; Willenbrock, F; Murphy, G. FEBS Letters 296,1992, 3, 263. b) The potency of compounds against wild type enzyme was determined using the procedure in Bickett, D. M; Green, M. D; Berman, J; Dezube, M; Howe, A. S; Brown, P. J; Roth, J. T; McGeehan, G. M; Anal. Biochem., 1993, 212, 58-63
20. 10. Groups of male rats (n=12) were dosed orally with the test compounds (10 mg/kg), serial blood samples were removed and MMPI activity extracted and assayed against HFC. Concentrations were calculated against a standard curve; Bone, E. A; Askew, M; Laber, D. unpublished results.