Bioorganic and Medicinal Chemistry Letters p. 1359 - 1364 (1998)
Update date:2022-08-05
Topics:
Pratt, Lisa M.
Beckett, R. Paul
Bellamy, Claire L.
Corkill, Dominic J.
Cossins, Judy
Courtney, Paul F.
Davies, Stephen J.
Davidson, Alan H.
Drummond, Alan H.
Helfrich, Karen
Lewis, Christopher N.
Mangan, Matthew
Martin, Fionna M.
Miller, Karen
Nayee, Prakash
Rickerts, Michelle L.
Thomas, Wayne
Todd, Richard S.
Whittaker, Mark
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 α-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 TNFα release.
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Doi:10.1016/S0022-328X(97)00627-X
(1998)Doi:10.1021/jo980097w
(1998)Doi:10.1016/S0040-4039(98)00494-8
(1998)Doi:10.1055/s-1998-1708
(1998)Doi:10.1021/acs.orglett.9b02408
(2019)Doi:10.1016/S0277-5387(97)00397-5
(1998)
