| Literature DB >> 9871766 |
L M Pratt1, R P Beckett, C L Bellamy, D J Corkill, J Cossins, P F Courtney, S J Davies, A H Davidson, A H Drummond, K Helfrich, C N Lewis, M Mangan, F M Martin, K Miller, P Nayee, M L Ricketts, W Thomas, R S Todd, M Whittaker.
Abstract
Matrix metalloproteinase inhibitors of general formula (1) were synthesised by a route involving an Ireland-Claisen rearrangement which enables systematic modification of the substituent alpha to the hydroxamic acid. An analogue (12c) possessing an alpha-cyclopentyl group is a potent broad spectrum inhibitor that displays high and sustained blood levels following oral dosing in both the rat and marmoset ex-vivo bioassays. This compound and analogues are also potent inhibitors of TNF alpha release.Entities:
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Year: 1998 PMID： 9871766 DOI： 10.1016/s0960-894x(98)00218-2
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823