24237-44-3Relevant articles and documents
New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds
Szántó, Gábor,Makó, Attila,Bata, Imre,Farkas, Bence,Kolok, Sándor,Vastag, Mónika,Cselenyák, Attila
, p. 3896 - 3904 (2016)
Purinergic P2X3 receptors are trimeric ligand-gated ion channels whose antagonism is an appealing yet challenging and not fully validated drug development idea. With the aim of identification of an orally active, potent human P2X3 receptor antagonist compound that can penetrate the central nervous system, the compound collection of Gedeon Richter was screened. A hit series of tricyclic compounds was subjected to a rapid, two-step optimization process focusing on increasing potency, improving metabolic stability and CNS penetrability. Attempts resulted in compound 65, a potential tool compound for testing P2X3 inhibitory effects in vivo.
Efficient three-component Gewald reactions under Et3N/H 2O conditions
Abaee, M. Saeed,Cheraghi, Somayeh
, p. 261 - 269 (2014/04/03)
In a medium consisting of triethylamine and water, methylene ketones undergo room temperature Gewald reactions with elemental sulfur and ethyl cyanoacetate (or malononitrile) to yield 2 aminothiophene derivatives efficiently within short time periods. Because of the high polarity of the medium, products precipitate in the reaction mixtures spontaneously. This makes isolation of the products easy by simple filtration and avoids cumbersome chromatographic separations. Mechanistic studies suggest that the reactions proceed via a Knoevenagel condensation pathway(equation presented). 2013
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors
Pinkerton, Anthony B.,Lee, Tom T.,Hoffman, Timothy Z.,Wang, Yan,Kahraman, Mehmet,Cook, Travis G.,Severance, Daniel,Gahman, Timothy C.,Noble, Stewart A.,Shiau, Andrew K.,Davis, Robert L.
, p. 3562 - 3569 (2008/12/23)
We have identified and synthesized a series of thiophene containing inhibitors of kinesin spindle protein. SAR studies led to the synthesis of 33, which was co-crystallized with KSP and determined to bind to an allosteric pocket previously described for o
