McGeary, Ross P. and Vella, Peter and Mak, Jeffrey Y. W. and Guddat, Luke W. and Schenk, Gerhard
Inhibition of purple acid phosphatase with a-alkoxynaphthylmethylphosphonic
Bioorganic and Medicinal Chemistry Letters , 19.
Purple acid phosphatases (PAPs) are binuclear hydrolases that catalyse the hydrolysis of a range of phosphorylated
substrates. Human PAP is a major histochemical marker for the diagnosis of osteoporosis. In
patients suffering from this disorder, PAP activity contributes to increased bone resorption and, therefore,
human PAP is a key target for the development of anti-osteoporotic drugs. This manuscript describes the
design and synthesis of derivatives of 1-naphthylmethylphosphonic acids as inhibitors of PAP. The Ki values
of these compounds are as low as 4 lM, the lowest reported to date for a PAP inhibitor.
||Purple acid phosphatase; PAP; Phosphonate;
||Science & Engineering > Chemistry
||31 May 2012 14:30
|Journal or Publication Title:
||Bioorganic and Medicinal Chemistry Letters
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