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

Kennedy JP, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2009 19 (12): 3204-8

PMID: 19443215 · PMCID: PMC4793969 · DOI:10.1016/j.bmcl.2009.04.106

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.

MeSH Terms (13)

Alkaloids Animals Biological Products Bromine Histamine H3 Antagonists Humans Inhibitory Concentration 50 Porifera Pyrroles Receptors, Histamine H3 Structure-Activity Relationship Sympathomimetics Tyramine

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