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https://doi.org/10.1016/j.bmcl.2009.08.052
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. Poon, T.-Y. Wong, P.T.H. Chui, W.-K. |
Keywords: | 2,4-Diamino-1,3,5-triazines Antiepilepsy Sodium channel blockers |
Issue Date: | 1-Oct-2009 | Citation: | 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 | URI: | http://scholarbank.nus.edu.sg/handle/10635/90267 | ISSN: | 0960894X | DOI: | 10.1016/j.bmcl.2009.08.052 |
Appears in Collections: | Staff Publications |
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