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Levin JI, Chen JM, Du MT, Nelson FC, Wehr T, DiJoseph JF, Killar LM, Skala S, Sung A, Sharr MA, Roth CE, Jin G, Cowling R, Di L, Sherman M, Xu ZB, March CJ, Mohler KM, Black RA, Skotnicki JS: The discovery of anthranilic acid-based MMP inhibitors. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2975-8.
Part 3: incorporation of basic amines.. Anthranilic acid derivatives bearing basic amines were prepared and evaluated in vitro and in vivo as inhibitors of MMP-1, MMP-9, MMP-13, and TACE. Piperazine 4u has been identified as a potent, selective, orally active inhibitor of MMP-9 and MMP-13. |
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