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|Title:||Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers|
|Authors:||Ma, X. |
Sodium channel blockers
|Source:||Ma, X., Poon, T.-Y., Wong, P.T.H., Chui, W.-K. (2009-10-01). Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers. Bioorganic and Medicinal Chemistry Letters 19 (19) : 5644-5647. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bmcl.2009.08.052|
|Abstract:||Neuronal sodium channels blockers interfere with ion flux and have been used for managing neuropathic pain, epilepsy, and cerebral ischemic disorders. In the current study, four groups of 2,4-diamino-1,3,5-triazine derivatives were synthesized and investigated for their neuronal sodium channels binding activity. 5-Aryl-1,3,5-triazaspiro[5.5]undeca-1,3-diene-2,4-diamines (4a-4j) were found to have the best neuronal sodium binding activity among the four groups of triazines evaluated. Derivatives 4a-4j blocked the sodium channels with IC50 values ranged from 4.0 to 14.7 μM. The result from this study showed that analogues of 2,4-diamino-1,3,5-triazines could be used as leads for the discovery of neuronal sodium channels blockers for managing central nervous system related disorders. © 2009 Elsevier Ltd. All rights reserved.|
|Source Title:||Bioorganic and Medicinal Chemistry Letters|
|Appears in Collections:||Staff Publications|
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