159054-14-5Relevant articles and documents
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists
Chen, Huayan,Yang, Hui,Wang, Zhilong,Xie, Xin,Nan, Fajun
, p. 335 - 339 (2016/03/25)
The indole derivative, 3-((E)-3-((3-((E)-2-(7-chloroquinolin-2yl)vinyl)phenyl)amino)-3-oxoprop-1-en-1-yl)-7-methoxy-1H-indole-2-carboxylic acid (17k), was identified as a novel and highly potent and selective CysLT1 antagonist with IC50 values of 0.0059 ± 0.0011 and 15 ± 4 μM for CysLT1 and CysLT2, respectively.
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site
Di Fabio, Romano,Capelli, Anna M.,Conti, Nadia,Cugola, Alfredo,Donati, Daniele,Feriani, Aldo,Gastaldi, Paola,Gaviraghi, Giovanni,Hewkin, Cheryl T.,Micheli, Fabrizio,Missio, Andrea,Mugnaini, Manolo,Pecunioso, Angelo,Quaglia, Anna M.,Ratti, Emiliangelo,Rossi, Luciana,Tedesco, Giovanna,Trist, David G.,Reggiani, Angelo
, p. 841 - 850 (2007/10/03)
A series of indole-2-carboxylates bearing suitable chains at the C-3 position of the indole nucleus was synthesized and evaluated in terms of in vitro affinity using [3H]glycine binding assay and in vivo potency by inhibition of convulsions ind