The synthesis of novel matrix metalloproteinase inhibitors employing the Ireland-Claisen rearrangement.
作者信息
Pratt L M, Beckett R P, Bellamy C L, Corkill D J, Cossins J, Courtney P F, Davies S J, Davidson A H, Drummond A H, Helfrich K, Lewis C N, Mangan M, Martin F M, Miller K, Nayee P, Ricketts M L, Thomas W, Todd R S, Whittaker M
机构信息
British Biotech Pharmaceuticals Limited, Cowley, Oxford.
出版信息
Bioorg Med Chem Lett. 1998 Jun 2;8(11):1359-64. doi: 10.1016/s0960-894x(98)00218-2.
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.
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