1069472-64-5Relevant articles and documents
UNNATURAL DISPYRIN ANALOGUES, PREPARATION AND USES THEREOF
-
, (2010/01/07)
Disclosed are dispyrin analogue compounds useful as H3 receptor activity modulators, methods of making same, pharmaceutical compositions comprising same, and methods of treating neurological and psychiatric disorders associated with histamine H3 receptor activity using same. In one aspect, the disclosed analogues can have a structure represented by a formula: (I), This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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.