474843-59-9Relevant 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 (2016/08/01)
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.
Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B
Andersen, Henrik Sune,Olsen, Ole H.,Iversen, Lars F.,S?rensen, Anette L. P.,Mortensen, Steen B.,Christensen, Michael S.,Branner, Sven,Hansen, Thomas K.,Lau, Jesper F.,Jeppesen, Lone,Moran, Edmond J.,Su, Jing,Bakir, Farid,Judge, Luke,Shahbaz, Manou,Collins, Tassie,Vo, Todd,Newman, Michael J.,Ripka, William C.,M?ller, Niels Peter H.
, p. 4443 - 4459 (2007/10/03)
Reversible phosphorylation and dephosphorylation of key proteins on tyrosine residues are important parts of intracellular signaling triggered by hormones and other agents. Recent knock-out studies in mice have identified PTP1B as a potential target for t
