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Journals and Conferences
Synthesis and structure-activity relationships (SAR) are described for a series of N,N'-diarylguanidines related to N-acenaphth-5-yl-N'-(4-methoxynaphth-1-yl)guanidine (3) as anticonvulsants through blockade of sodium channels. SAR studies on compound 3 led to several simpler diphenylguanidines with improved in vitro and in vivo activity. Compounds were… (More)
Solution-phase synthesis of various acylguanidine derivatives and the evaluation of a small library of compounds as potential sodium channel blockers are described.
Radioligand binding techniques were used to determine the affinity of a series of substituted guanidine derivatives for 1) the binding site within the ion channel of the N-methyl-D-aspartate (NMDA) receptor, as defined by displacement of MK-801 ([3H]dizocilpine) and 2) sigma sites as defined by displacement of [3H]N,N'-di-(o-tolyl)guanidine. The goal was to… (More)