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

Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.

Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of biphenylsulfonamidocarboxylic acid inhibitors of aggrecanase-1 are reported. Compound 24 demonstrated 89% inhibition of proteoglycan degradation at 10 microg/mL and has an oral bioavailability in rat of 35%.[1]

References

  1. Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors. Xiang, J.S., Hu, Y., Rush, T.S., Thomason, J.R., Ipek, M., Sum, P.E., Abrous, L., Sabatini, J.J., Georgiadis, K., Reifenberg, E., Majumdar, M., Morris, E.A., Tam, S. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
 
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