Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers |
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Authors: | Xiang Ma Thong-Yuen Poon Peter Tsun Hon Wong Wai-Keung Chui |
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Institution: | 1. Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore;2. Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive, Singapore 117576, Singapore;3. Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, 10 Medical Drive, Singapore 117597, Singapore |
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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-triazaspiro5.5]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. |
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