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Bioorg Med Chem Lett. 2009 Jun 15;19(12):3204-8. doi: 10.1016/j.bmcl.2009.04.106. Epub 2009 May 3.

A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.

Author information

1
Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA.

Abstract

This Letter describes the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin, and the resulting SAR of H(3) antagonism. Multiple rounds of iterative parallel synthesis improved human H(3) IC(50) approximately 33-fold, and afforded a new class of H(3) antagonists based on the novel bromotyramine core of dispyrin.

PMID:
19443215
PMCID:
PMC4793969
DOI:
10.1016/j.bmcl.2009.04.106
[Indexed for MEDLINE]
Free PMC Article

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