- Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents
-
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.
- Yang, Shaoning,Lu, Dingqiang,Ouyang, Pingkai
-
supporting information
p. 1731 - 1735
(2018/05/04)
-
- Superacid-catalyzed preparation of aryl-substituted piperidines via dicationic electrophiles
-
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
- Klumpp, Douglas A.,Beauchamp, Philip S.,Sanchez Jr., Gregorio V.,Aguirre, Sharon,De Leon, Sarah
-
p. 5821 - 5823
(2007/10/03)
-
- SYNTHESE ET ACTIVITE ANTI-DEPRESSIVE POTENTIELLE DE NOUVELLES TRIAZINE-1,2,3-ONES-4
-
Synthesis of new 1,2,3-triazin-4-ones as potential anti-depressants.A series of 1,2,3-triazin-4-ones was prepared and examined for potential anti-depressive activity by comparison with trazodone 2.Several of them show a potentiation of the central effects
- Ferrand, Gerard,Dumas, Herve,Depin, Jean-Claude,Chavernac, Gilles
-
p. 337 - 346
(2007/10/02)
-
