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Synthesis and quantitative structure-activity relationships of anticonvulsant 2, 3, 6-triaminopyridines

JK Seydel, KJ Schaper, EA Coats…

文献索引:Seydel; Schaper; Coats; Cordes Journal of Medicinal Chemistry, 1994 , vol. 37, # 19 p. 3016 - 3022

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被引用次数: 29

摘要

The synthesis of 2, 3, 6-triaminopyridine derivatives, representing a unique chemical structure for anticonvulsants, is described. The synthetic program was performed (a) to identify more potent analogs,(b) to determine structural properties controlling potency as well as neurotoxicity, and (c) to reduce the requirements for animal testing. As a result, besides other structural properties, the overall molecular lipophilicity (log k', octanol- ...