186797-08-0Relevant academic research and scientific papers
First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold
Cheng, Hei Wun Alison,Sokias, Renee,Werry, Eryn L.,Ittner, Lars M.,Reekie, Tristan A.,Du, Jonathan,Gao, Quanqing,Hibbs, David E.,Kassiou, Michael
supporting information, p. 8235 - 8248 (2019/10/11)
Development of neuroinflammation agents targeting the translocator protein (TSPO) has been hindered by a common single nucleotide polymorphism (A147T) at which TSPO ligands commonly lose affinity. To this end, carbazole acetamide scaffolds were synthesized and structure activity relationships elaborated to explore the requirements for high-affinity binding to both TSPO wild type (WT) and the polymorphic TSPO A147T. This study reports high binding affinity and nondiscriminating TSPO ligands.
Facile synthesis of 4-substituted 1,2,4,5-tetrahydro-1,4-benzodiazepin-3-ones by reductive cyclization of 2-chloro-N-(2-nitrobenzyl)acetamides
Sasiambarrena, Leandro D.,Barri, Ivan A.,Fraga, Guido G.,Bravo, Rodolfo D.,Ponzinibbio, Agustín
supporting information, p. 264 - 267 (2019/01/04)
A facile and efficient method was developed for the synthesis of 1,2,4,5-tetrahydro-1,4-benzodiazepine-3-ones from 2-chloro-N-(2-nitrobenzyl)acetamides through a reductive cyclization using iron-ammonium chloride in ethanol–water in good yields. This method provides a simple approach to these benzodiazepine-3-ones which are of high value in the field of medicinal chemistry research.
Quinazolinones, Quinazolinthiones, and Quinazolinimines as Nitric Oxide Synthase Inhibitors: Synthetic Study and Biological Evaluation
Camacho, M. Encarnación,Chayah, Mariem,García, M. Esther,Fernández-Sáez, Nerea,Arias, Fabio,Gallo, Miguel A.,Carrión, M. Dora
, p. 638 - 650 (2016/08/27)
The synthesis of different compounds with a quinazolinone, quinazolinthione, or quinazolinimine skeleton and their in vitro biological evaluation as inhibitors of inducible and neuronal nitric oxide synthase (iNOS and nNOS) isoforms are described. These d
Substituted aryl and heteroaryl compounds as E-type prostaglandin antagonists
-
, (2008/06/13)
This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula STR1 and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.
