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ID: ALA1139252

Journal: Bioorg Med Chem Lett

Title: Inhibition of purple acid phosphatase with alpha-alkoxynaphthylmethylphosphonic acids.

Authors: McGeary RP, Vella P, Mak JY, Guddat LW, Schenk G.

Abstract: 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 K(i) values of these compounds are as low as 4 microM, the lowest reported to date for a PAP inhibitor.

CiteXplore: 19010677

DOI: 10.1016/j.bmcl.2008.10.125