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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.

Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-alpha release. Oral activity in the mouse LPS model of TNF-alpha release was seen. Efficacy in the mouse collagen induced arthritis model was achieved with diazepine 20.[1]

References

  1. Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors. Zask, A., Kaplan, J., Du, X., MacEwan, G., Sandanayaka, V., Eudy, N., Levin, J., Jin, G., Xu, J., Cummons, T., Barone, D., Ayral-Kaloustian, S., Skotnicki, J. Bioorg. Med. Chem. Lett. (2005) [Pubmed]
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