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The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors. |
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| Authors: | F M Martin R P Beckett C L Bellamy P F Courtney S J Davies A H Drummond R Dodd L M Pratt S R Patel M L Ricketts R S Todd A R Tuffnell J W Ward M Whittaker |
| Affiliation: | British Biotech Pharmaceuticals Limited, Cowley, Oxford. martinf@britbio.co.uk |
| Abstract: |  Novel sulfonamide matrix metalloproteinase inhibitors of general formula (9) were synthesised by a route involving a stereoselective conjugate addition reaction. Enzyme selectivity was found to be dependant on the nature of the sulfonamide substituents. Compounds (9f, 9q) are potent selective collagenase inhibitors with good oral bioavailability. |
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