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Bioorg Med Chem Lett. 2010 Oct 15;20(20):6157-60. doi: 10.1016/j.bmcl.2009.05.077. Epub 2009 May 24.

A class of novel conjugates of substituted purine and Gly-AA-OBzl: synthesis and evaluation of orally analgesic activity.

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1
College of Pharmaceutical Sciences, Peking University, Beijing, PR China.

Abstract

Aimed at the chemotherapy of chronic pain two kinds of analgesic pharmacophores, substituted purine and Gly-AA-OBzl, were coupled via a five-step-reaction procedure and 19 novel conjugates N-[2-chloro-9-(tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters were provided. On mouse-tail flick model their in vivo analgesic activities were assayed. The results indicate that introducing Gly-OC(2)H(5) into the 6-position of the substituted purine leads to ambiguous increase of the analgesic activity, while introducing Gly-AA-OBzl into this position leads to significant increase of the analgesic activity.

PMID:
20833035
DOI:
10.1016/j.bmcl.2009.05.077
[Indexed for MEDLINE]
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