180161-17-5Relevant articles and documents
20-HETE FORMATION INHIBITORS
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Paragraph 0357-0360; 0393; 0394, (2020/08/23)
This disclosure provides novel heterocyclic compounds and methods for inhibiting the enzyme CYP4. Further disclosed methods include: a method of inhibiting the biosynthesis of 20-hydroxyeicosatetraenoic acid (20-HETE) in a subject in need thereof and a method of producing neuroprotection and decreased brain damage by preventing cerebral microvascular blood flow impairment and anti-oxidant mechanisms in a subject experiencing or having experienced an ischemic event.
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents
Yang, Shaoning,Lu, Dingqiang,Ouyang, Pingkai
supporting information, p. 1731 - 1735 (2018/05/04)
Epilepsy is a kind of disease with complicated pathogenesis. KCNQ (Kv7) is a voltage dependent potassium channel that is mostly associated with epilepsy and thus becomes an important target in the treatment of epilepsy. In this paper, a series of substituted piperidine derivatives targeting KCNQ were designed and synthesized by using scaffold hopping and active substructure hybridization. Compounds were evaluated by fluorescence-based thallium influx assay, Rb+ flow assay and electrophysiological patch-clamp assay. Results showed that some compounds possessed more potent potassium channel opening activity than Retigabine. More significantly, compound 11 was found to have good pharmacokinetic profiles in vivo.
Superacid-catalyzed preparation of aryl-substituted piperidines via dicationic electrophiles
Klumpp, Douglas A.,Beauchamp, Philip S.,Sanchez Jr., Gregorio V.,Aguirre, Sharon,De Leon, Sarah
, p. 5821 - 5823 (2007/10/03)
The electrophilic chemistry of 1,2,3,6-tetrahydropyridines has been studied in the Bronsted superacid, CF3SO3H (triflic acid). The 1,2,3,6-tetrahydropyridines react with arenes to give aryl-substituted piperidines. It is proposed tha