138647-50-4Relevant articles and documents
TRPML MODULATORS
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Paragraph 0314, (2021/06/26)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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.
METALLO-BETA-LACTAMASE INHIBITORS
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Paragraph 0784, (2016/12/01)
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.