A novel class of H-3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin

[摘要]：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 IC50 similar to 33-fold, and afforded a new class of H-3 antagonists based on the novel bromotyramine core of dispyrin. (C) 2009 Elsevier Ltd. All rights reserved.

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