The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.

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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. Part 3: incorporation of basic amines.

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2975-8.

PubMed ID

11677139 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
WAY-151693	Collagenase 3	IC 50 (nM)	8	N/A	N/A	Details
WAY-151693	Collagenase 3	IC 50 (nM)	18	N/A	N/A	Details