1069472-65-6Relevant academic research and scientific papers
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: Elucidation of discrete molecular targets with therapeutic potential
Kennedy, J. Phillip,Brogan, John T.,Lindsley, Craig W.
experimental part, p. 1783 - 1786 (2009/07/11)
The first total synthesis of dispyrin, a recently reported bromopyrrole alkaloid from Agelas dispar with an unprecedented bromopyrrole tyramine motif, was achieved in three steps on a gram scale (68.4% overall). No biological activity was reported for dispyrin, so we evaluated synthetic dispyrin against >200 discrete molecular targets in radioligand binding and functional assays. Unlike most marine natural products, dispyrin (1) possesses no antibacterial or anticancer activity, but was found to be a potent ligand and antagonist of several therapeutically relevant GPCRs, the α1D and α2A adrenergic receptors and the H2 and H3 histamine receptors.
