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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

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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 Ki values of these compounds are as low as 4 lM, the lowest reported to date for a PAP inhibitor.

Item Type: Article
Keywords: Purple acid phosphatase; PAP; Phosphonate;
Subjects: Science & Engineering > Chemistry
Item ID: 3719
Depositing User: Gary Schenk
Date Deposited: 31 May 2012 14:30
Journal or Publication Title: Bioorganic and Medicinal Chemistry Letters
Publisher: Elsevier
Refereed: Yes
URI:

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