Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmcl.2009.08.052
DC FieldValue
dc.titleSynthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers
dc.contributor.authorMa, X.
dc.contributor.authorPoon, T.-Y.
dc.contributor.authorWong, P.T.H.
dc.contributor.authorChui, W.-K.
dc.date.accessioned2014-10-09T07:03:17Z
dc.date.available2014-10-09T07:03:17Z
dc.date.issued2009-10-01
dc.identifier.citationMa, 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
dc.identifier.issn0960894X
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/90267
dc.description.abstractNeuronal 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.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/j.bmcl.2009.08.052
dc.sourceScopus
dc.subject2,4-Diamino-1,3,5-triazines
dc.subjectAntiepilepsy
dc.subjectSodium channel blockers
dc.typeArticle
dc.contributor.departmentPHARMACY
dc.contributor.departmentCHEMICAL & BIOMOLECULAR ENGINEERING
dc.description.doi10.1016/j.bmcl.2009.08.052
dc.description.sourcetitleBioorganic and Medicinal Chemistry Letters
dc.description.volume19
dc.description.issue19
dc.description.page5644-5647
dc.description.codenBMCLE
dc.identifier.isiut000270106700027
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