33543-95-2

Upstream product

• 6921-64-8 4'-hydroxy-2'-methylacetophenone 
• 95-92-1 oxalic acid diethyl ester 
• 108-39-4 3-methyl-phenol 
• 762-21-0 acetylenedicarboxylic acid diethyl ester 

Downstream Products

• 33543-96-3 2-carbamyl-7-methyl-4-oxo-4H-1-benzopyran 
• 823805-53-4 (2,9-dimethyl-3,4,5,6-tetrahydro-2H-benzo[b]oxocin-2-yl)-methanol 
• 823805-56-7 2,2,9-trimethyl-2,3,4,5-tetrahydro-benzo[b]oxocin-6-one 

Relevant academic research and scientific papers

A novel synthetic compound MCAP suppresses LPS-induced murine microglial activation in vitro via inhibiting NF-kB and p38 MAPK pathways

Aim: To investigate the anti-neuroinflammatory activity of a novel synthetic compound, 7-methylchroman-2-carboxylic acid N-(2-trifluoromethyl) phenylamide (MCAP) against LPS-induced microglial activation in vitro.Methods:Primary mouse microglia and BV2 microglia cells were exposed to LPS (50 or 100 ng/mL). The expression of iNOS and COX-2, proinflammatory cytokines, NF-κB and p38 MAPK signaling molecules were analyzed by RT-PCR, Western blot and ELISA. The morphological changes of microglia and nuclear translocation of NF-κB were visualized using phase contrast and fluorescence microscopy, respectively. Results: Pretreatment with MCAP (0.1, 1, 10 μmol/L) dose-dependently inhibited LPS-induced expression of iNOS and COX-2 in BV2 microglia cells. Similar results were obtained in primary microglia pretreated with MCAP (0.1, 0.5 μmol/L). MCAP dose-dependently abated LPS-induced release of TNF-α, IL-6 and IL-1β, and mitigated LPS-induced activation of NF-κB by reducing the phosphorylation of IκBα in BV2 microglia cells. Moreover, MCAP attenuated LPS-induced phosphorylation of p38 MAPK, whereas SB203580, a p38 MAPK inhibitor, significantly potentiated MCAP-caused inhibition on the expression of MEF-2 (a transcription factor downstream of p38 MAPK). Conclusion: MCAP exerts anti-inflammatory effects in murine microglia in vitro by inhibiting the p38 MAPK and NF-κB signaling pathways and proinflammatory responses. MCAP may be developed as a novel agent for treating diseases involving activated microglial cells.

SUBSTITUTED CYCLOLAKYLS AS MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.

An efficient construction of 4-OXO-4H-chromene-2-carboxylate derivatives via one-pot cascade reaction under solvent-free conditions

An efficient synthetic strategy to chromone derivatives from commercially available diethyl acetylenedicarboxylate and phenols via a one-pot cascade reaction has been developed. Performing the reaction using pyridine and polyphosphoric acid as the catalyst at room temperature and 90°C without any solvent gave the chromone derivatives in good to high yields at one time. A possible reaction pathway was also proposed and supported by the experiment. This protocol is environmentally friendly and metal-free, with advantages including short reaction times, convenient operation, and mild reaction conditions.

Facile transfer hydrogenation of chromones

Refluxing a solution of chromones in methanol containing ammonium formate and Pd-C leads to facile hydrogenation to chromanones.

QUINOLINYL-BENZOPYRAN DERIVATIVES AS ANTAGONISTS OF LEUKOTRIENE D4

This invention relates to certain quinolinyl-benzopyran compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists and/or mediator release inhibitors possessing anti-inflammatory and anti-allergic properties.

QUINOLINYL-CHROMONE DERIVATIVES AND USE FOR TREATMENT OF HYPERSENSITIVE AILMENTS

This invention relates to certain quinolinyl-chromone compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists possessing anti-inflammatory and anti-allergic properties.