181220-75-7Relevant academic research and scientific papers
Novel and selective TLR7 antagonists among the imidazo[1,2- a]pyrazines, Imidazo[1,5- a]quinoxalines, and Pyrazolo[1,5- a]quinoxalines Series
Bou Karroum, Nour,Moarbess, Georges,Guichou, Jean-Fran?ois,Bonnet, Pierre-Antoine,Patinote, Cindy,Bouharoun-Tayoun, Hasnaa,Chamat, Soulaima,Cuq, Pierre,Diab-Assaf, Mona,Kassab, Issam,Deleuze-Masquefa, Carine
, p. 7015 - 7031 (2019)
The Toll-like receptors (TLRs) 7 and 8 play an important role in the immune system activation, and their agonists may therefore serve as promising candidate vaccine adjuvants. However, the chronic immune activation by excessive TLR stimulation is a hallmark of several clinically important infectious and autoimmune diseases, which warrants the search for TLR antagonists. In this study, we have synthesized and characterized a variety of compounds belonging to three heterocyclic chemical series: imidazo[1,2-a]pyrazine, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline. These compounds have been tested for their TLR7 or TLR8 agonistic and antagonistic activities. Several of them are shown to be selective TLR7 antagonists without any TLR7 or TLR8 agonistic activity. The selectivity was confirmed by a comparative ligand-docking study in TLR7 antagonist pocket. Two compounds of the pyrazolo[1,5-a]quinoxaline series (10a and 10b) are potent selective TLR7 antagonists and may be considered as promising starting points for the development of new therapeutic agents.
FACTOR XIa INHIBITORS
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Page/Page column 126, (2015/12/09)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
FRICTIONLESS MOLECULAR ROTARY MOTORS
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Page/Page column 29, (2010/02/17)
A rotaxane consisting of a cucurbituril and an uncharged guest molecule, having low or null affinity therebetween is provided as well as processes for providing the same. Various uses as energy converters (“frictionless” molecular motors), biochips and biosensors using the same are also provided.
