359804-46-9Relevant academic research and scientific papers
Synthesis and: In vitro evaluation of fluorine-18 benzimidazole sulfones as CB2 PET-radioligands
Kallinen, Annukka,Boyd, Rochelle,Lane, Samuel,Bhalla, Rajiv,Mardon, Karine,Stimson, Damion H. R.,Werry, Eryn L.,Fulton, Roger,Connor, Mark,Kassiou, Michael
, p. 5086 - 5098 (2019/06/03)
Cannabinoid type 2 receptor (CB2) is up-regulated on activated microglial cells and can potentially be used as a biomarker for PET-imaging of neuroinflammation. In this study the synthesis and pharmacological evaluation of novel fluorinated pyridyl and et
The fight against the influenza A virus H1N1: Synthesis, molecular modeling, and biological evaluation of benzofurazan derivatives as viral RNA polymerase inhibitors
Pagano, Mafalda,Castagnolo, Daniele,Bernardini, Martina,Fallacara, Anna Lucia,Laurenzana, Ilaria,Deodato, Davide,Kessler, Ulrich,Pilger, Beatrice,Stergiou, Lilli,Strunze, Stephan,Tintori, Cristina,Botta, Maurizio
, p. 129 - 150 (2014/01/17)
The influenza RNA polymerase complex, which consists of the three subunits PA, PB1, and PB2, is a promising target for the development of new antiviral drugs. A large library of benzofurazan compounds was synthesized and assayed against influenza virus A/WSN/33 (H1N1). Most of the new derivatives were found to act by inhibiting the viral RNA polymerase complex through disruption of the complex formed between subunits PA and PB1. Docking studies were also performed to elucidate the binding mode of benzofurazans within the PB1 binding site in PA and to identify amino acids involved in their mechanism of action. The predicted binding pose is fully consistent with the biological data and lays the foundation for the rational development of more effective PA-PB1 inhibitors. In the fight against influenza virus A/WSN/33 (H1N1), the PA-PB1 protein-protein interaction is emerging as a new drug target. To identify small molecules able to inhibit the viral RNA polymerase complex, the benzofurazan scaffold was explored by synthesizing a large library of derivatives. Some compounds showed high anti-H1N1 activity and emerged as effective inhibitors of the PA-PB1 interaction, with IC50 values in the micromolar range. Copyright
BENZIMIDAZOLE CANNABINOID AGONISTS BEARING A SUBSTITUTED HETEROCYCLIC GROUP
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Paragraph 0102; 0103; 0104, (2014/01/07)
The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
5-Sulfonyl-benzimidazoles as selective CB2 agonists-Part 2
Gijsen, Harrie J.M.,De Cleyn, Michel A.J.,Surkyn, Michel,Van Lommen, Guy R.E.,Verbist, Bie M.P.,Nijsen, Marjoleen J.M.A.,Meert, Theo,Wauwe, Jean Van,Aerssens, Jeroen
scheme or table, p. 547 - 552 (2012/03/11)
In a previous communication, the SAR of a series of potent and selective 5-sulfonyl-benzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their poor solubility and metabolic stabili
FLUOROALKYL SUBSTITUTED BENZIMIDAZOLE CANNABINOID AGONISTS
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Page/Page column 13, (2009/07/18)
The present invention is related to benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the trea
BENZIMIDAZOLE CANNABINOID AGONISTS BEARING A SUBSTITUTED HETEROCYCLIC GROUP
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Page/Page column 18, (2008/06/13)
The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
5-Sulfonyl-benzimidazoles as selective CB2 agonists
Verbist, Bie M.P.,De Cleyn, Michel A.J.,Surkyn, Michel,Fraiponts, Erwin,Aerssens, Jeroen,Nijsen, Marjoleen J.M.A.,Gijsen, Harrie J.M.
, p. 2574 - 2579 (2008/12/21)
A novel series of benzimidazole CB2-receptor agonists was synthesized and the structure-activity relationship explored. The results showed agonistic activities with an EC50 up to 0.5 nM and excellent selectivity (>4000-fold) over the CB1 receptor. The size of the substituent on the 2-position determined the level of agonism, ranging from inverse agonism to partial agonism to full agonism, which was more pronounced for the rat CB2 receptor. A wide variation of sulfonyl substituents at the benzimidazole 5-position was tolerated, which was used to optimize the drug-like properties. This resulted into lead compound 14j that can be used to investigate the potential of a selective, peripherically acting CB2 agonist. The in vitro profile of key compounds is displayed using pie bar charts (VlaaiVis).
BENZIMIDAZOLE CANNABINOID AGONISTS
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Page/Page column 19, (2008/12/04)
The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in th
