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

[img] Download (461kB)


Share your research

Twitter Facebook LinkedIn GooglePlus Email more...



Add this article to your Mendeley library


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;
Academic Unit: Faculty of Science and 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:

Repository Staff Only(login required)

View Item Item control page

Document Downloads

More statistics for this item...