rdf:type |
|
lifeskim:mentions |
umls-concept:C0002062,
umls-concept:C0181090,
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0243071,
umls-concept:C0243076,
umls-concept:C0302614,
umls-concept:C0456387,
umls-concept:C0679622,
umls-concept:C1441547,
umls-concept:C1566558,
umls-concept:C1706050,
umls-concept:C1883254,
umls-concept:C1957023
|
pubmed:issue |
12
|
pubmed:dateCreated |
2009-5-29
|
pubmed:abstractText |
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.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
1464-3405
|
pubmed:author |
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
19
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3204-8
|
pubmed:dateRevised |
2011-11-17
|
pubmed:meshHeading |
pubmed-meshheading:19443215-Alkaloids,
pubmed-meshheading:19443215-Animals,
pubmed-meshheading:19443215-Biological Agents,
pubmed-meshheading:19443215-Bromine,
pubmed-meshheading:19443215-Histamine H3 Antagonists,
pubmed-meshheading:19443215-Humans,
pubmed-meshheading:19443215-Inhibitory Concentration 50,
pubmed-meshheading:19443215-Porifera,
pubmed-meshheading:19443215-Pyrroles,
pubmed-meshheading:19443215-Receptors, Histamine H3,
pubmed-meshheading:19443215-Structure-Activity Relationship,
pubmed-meshheading:19443215-Sympathomimetics,
pubmed-meshheading:19443215-Tyramine
|
pubmed:year |
2009
|
pubmed:articleTitle |
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.
|
pubmed:affiliation |
Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|