Inhibition of purple acid phosphatase with a-alkoxynaphthylmethylphosphonic acids
McGeary, Ross P. and Vella, Peter and Mak, Jeffrey Y. W. and Guddat, Luke W. and Schenk, Gerhard (2009) Inhibition of purple acid phosphatase with a-alkoxynaphthylmethylphosphonic acids. Bioorganic and Medicinal Chemistry Letters , 19 . pp. 163-166. ISSN 0960-894X
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.
Repository Staff Only: item control page