29668-44-8Relevant articles and documents
Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents
Sun, Juan,Wang, Su,Sheng, Gui-Hua,Lian, Zhi-Min,Liu, Han-Yu,Zhu, Hai-Liang
, p. 5626 - 5632 (2016)
1-((2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-substituted-phenylpiperazine moiety was prepared and has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The biological activity of compound 3k as anti-inflammatory agent was further investigated both in vitro and in vivo. Notably, compound 3k exhibited the best anti-inflammatory activity among the eleven designed compounds with no toxicity, as determined by the ulcerogenic activity. Computational docking studies also showed that compound 3k has interaction with COX-2 key residues in the active site. Compound 3k maybe a new anti-inflammatory lead-candidate as powerful and novel non-ulcerogenic.
CONDENSED HETEROCYCLIC COMPOUND HAVING 1,4-BENZO DIOXANE RING OR SALT THEREOF, AND ANTI-JUVENILE HORMONE AGENT COMPOSED OF THE COMPOUND
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Paragraph 0015; 0033, (2020/02/28)
PROBLEM TO BE SOLVED: To provide a pest control agent containing a practical juvenile hormone antagonist activity compound as an active ingredient. SOLUTION: By using a reporter gene assay system that uses a juvenile hormone sequence, a heterocyclic compound having an antagonist activity is discovered, and a pest control agent containing the compound as an active ingredient is provided. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT
Synthesis, characterization, and docking studies of novel cyanopyridone analogs with serotonin 5-HT1B receptor agonists
Baitha, Amresh,Upadhyay, Manish,Gopinathan, Ajay,Krishnan, Karthik,Dabholkar, Vijay V.
supporting information, p. 844 - 851 (2019/03/26)
The medications in use for treating migraine are directed either towards inhibiting the characteristic migraine pain or towards preventing it from occurring. In this pursuit, ergotamine and sumatriptan class of 5-HT1B receptor agonists have been proved to be extremely effective. Further research into this field led us to design cyanopyridone derivatives that were synthesized through cyclization of 2-cyano-N-phenylacetamides with malonitrile and 2,3-dihydrobenzo[b][1,4]dioxine-6-carbaldehyde. The synthesized cyanopyridones analogs, when docked with active site of 5-HT1B receptor, showed better binding affinity compared to standard antimigraine medications. Additionally, in silico ADME prediction for drug-likeness and pharmacokinetics revealed that all compounds are safer and can be used as antimigraine medicine. The structure of the synthesized compounds has been elucidated on the basis of spectral analysis.