28355-48-8Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
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Paragraph 00555-00557, (2021/09/04)
The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
A directing group-assisted ruthenium-catalyzed approach to access: Meta -nitrated phenols
Sasmal, Sheuli,Sinha, Soumya Kumar,Lahiri, Goutam Kumar,Maiti, Debabrata
, p. 7100 - 7103 (2020/07/14)
meta-Selective C-H nitration of phenol derivatives was developed using a Ru-catalyzed σ-activation strategy. Cu(NO3)2·3H2O was employed as the nitrating source, whereas Ru3(CO)12 was found to be the most suitable metal catalyst for the protocol. Mechanistic studies suggested involvement of an ortho-CAr-H metal intermediate, which promoted meta-electrophilic aromatic substitution and silver-assisted free-radical pathway.
2-{2-[3-(Pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl}pyridine: A highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
Huang, Dehua,Poon, Steve F.,Chapman, Deborah F.,Chung, Janice,Cramer, Merryl,Reger, Thomas S.,Roppe, Jeffrey R.,Tehrani, Lida,Cosford, Nicholas D.P.,Smith, Nicholas D.
, p. 5473 - 5476 (2007/10/03)
Structure-activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2- yl)benzonitrile 2 led to the discovery of 2-{2-[3-(pyridin-3-yloxy)phenyl]-2H- tetrazol-5-yl}pyridine (10)-a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability. Structure-activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery of 2-{2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl}pyridine (10)-a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability.
N- and N- Sulfonamides: Potent Orally Active Leukotriene D4 Antagonists of Novel Structurs
Musser, John H.,Kreft, Anthony F.,Bender, Reinhold H. W.,Kubrak, Dennis M.,Carlson, Richard P.,et al.
, p. 1176 - 1183 (2007/10/02)
Two series of compounds, N- sulfonamides and N- sulfonamides, were prepared as leukotriene D4 (LTD4) antagonists.In the phenyl series, N--trifluoromethanesulfonamide (Wy-48,252, 16) was the most potent inhibitor of LTD4-induced bronchoconstriction in the guinea pig.With an intragastric ID 50 of 0.1 mg/kg (2-h pretreatment), 16 was 300 times more potent than LY-171,883.Compound 16 also intragastrically inhibited ovalbumin-induced bronchoconstriction in the guinea pig with an ID 50 of 0.6mg/kg.In vitro against LTD4-induced contraction of isolated guinea pig trachea pretreated with indomethacin and L-cysteine, 16 produced a pKB value of 7.7.In the rat PMN assay 16 inhibited both 5-lipoxygenase and cyclooxygenase (IC 50's = 4.6 and 3.3 μM).In the naphthyl series, N-trifluoromethanesulfonamide (Wy-48,090, 47) in addition to potent LTD4 antagonist activity (on isolated guinea pig trachea 47 had a pKB value of 7.04) also had antiinflammatory activity (63percent inhibition at 50 mg/kg in the rat carrageenan paw edema assay and 34percent inhibition of TPA-induced inflammation at 1 mg/ear in the mouse ear edema model).Perhaps the antiinflammatory activity of 47 was due to its additional activity of inhibiting both 5-lipoxygenase and cyclooxygenase enzymes (IC 50's = 0.23 and 11.9 μM, respectively, in rat PMN).
