2561-25-3Relevant articles and documents
HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF EPILEPSY
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Paragraph 0134; 0143; 0144, (2020/06/19)
The present invention provides a novel heterocyclic compound represented by Formula [I] and a salt thereof: wherein the symbols are as defined in the specification, which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.
Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels
Sairaman, Anjali,Cardoso, Fernanda Caldas,Bispat, Anjie,Lewis, Richard J.,Duggan, Peter J.,Tuck, Kellie L.
supporting information, p. 3046 - 3059 (2018/04/06)
Both N- and T-type calcium ion channels have been implicated in pain transmission and the N-type channel is a well-validated target for the treatment of neuropathic pain. An SAR investigation of a series of substituted aminobenzothiazoles identified a subset of five compounds with comparable activity to the positive control Z160 in a FLIPR-based intracellular calcium response assay measuring potency at both CaV2.2 and CaV3.2 channels. These compounds may form the basis for the development of drug leads and tool compounds for assessing in vivo effects of variable modulation of CaV2.2 and CaV3.2 channels.
Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors
Yang, Liuqing,Liu, Wei,Mei, Hanbing,Zhang, Yuan,Yu, Xiaojuan,Xu, Yufang,Li, Honglin,Huang, Jin,Zhao, Zhenjiang
supporting information, p. 671 - 676 (2015/04/27)
Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs. This journal is