313398-24-2Relevant academic research and scientific papers
HETEROARYL INHIBITORS OF PAD4
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, (2018/03/28)
The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists
Acker, Timothy M.,Khatri, Alpa,Vance, Katie M.,Slabber, Cathryn,Bacsa, John,Snyder, James P.,Traynelis, Stephen F.,Liotta, Dennis C.
supporting information, p. 6434 - 6456 (2013/09/23)
Here we describe the synthesis and structure-activity relationship for a class of pyrazoline-containing dihydroquinolone negative allosteric modulators of the NMDA receptor that show strong subunit selectivity for GluN2C- and GluN2D-containing receptors over GluN2A- and GluN2B-containing receptors. Several members of this class inhibit NMDA receptor responses in the nanomolar range and are more than 50-fold selective over GluN1/GluN2A and GluN1/GluN2B NMDA receptors, as well as AMPA, kainate, GABA, glycine, nicotinic, serotonin, and purinergic receptors. Analysis of the purified enantiomers of one of the more potent and selective compounds shows that the S-enantiomer is both more potent and more selective than the R-enantiomer. The S-enantiomer had an IC 50 of 0.17-0.22 μM at GluN2D- and GluN2C-containing receptors, respectively, and showed over 70-fold selectivity over other NMDA receptor subunits. The subunit selectivity of this class of compounds should be useful in defining the role of GluN2C- and GluN2D-containing receptors in specific brain circuits in both physiological and pathophysiological conditions.
Microwave assisted Friedlaender condensation: A comparative study of conventional versus microwave mediated solvent-free methodologies
Agrawal,Joshipura, Hardik M.
, p. 1649 - 1652 (2007/10/03)
4-Arylquinolines have been prepared by Friedlaender reaction with acid as a catalyst and without the catalyst under microwave assisted solvent-free conditions and compared with classical heating.
A new approach to the synthesis of benzo[b][1,8]naphthyridin-4(1h)ones
Vijayalakshmi,Ragunath,Rajendran
, p. 177 - 180 (2007/10/03)
Condensation of 3-acetyl-4-phenylquinoline-2(1H)ones 1 with benzaldehydes give 4-phenyl-3-cinnamoylquinolin-2(1H)ones 2 which inturn were converted to 2-chloro-3-cinnamoyl-4-phenylquinolines. 3. Compounds 3 were then aminated with p-aminobenzensulfonamide and then subjected to bromination-dehydrobromination step to yield 2.5-diphenylbenzo[b][1,8]naphthyridin-4(1H)ones 5.
