Comparison of anticonvulsive properties of eboracin and phenytoin in mice

The in vivo effects of phenytoin (diphenylhydantoin, Dilantin) and the experimental anticonvulsant, eboracin, a substituted indenopyrrole, were compared in mice. Pretreatment with varying dosages of either agent followed by challenge with the chemoconvulsant pentylenetetrazol (Metrazol) indicated that eboracin provided slightly less protection against seizures than phenytoin and was much less toxic. Intermediate doses of either agent led to a form of clonic status epilepticus which persisted for an average of 18 min in phenytoin-treated and 58 min in eboracin-treated mice. Pretreatment with higher or lower doses did not lead to these manifestations. Animals in which this syndrome had been induced should be of value in studies of the chemistry and physiology of the clonic state.     

Synthesis and search for anticonvulsive and hypoglycemic properties of novel 5-benzylidene derivatives of 3-o-chloro- and 3-o-methylbenzoyl-2-thiohydantoin

14 new benzylidene derivatives of 3-o-chloro- and 3-o-methylbenzoyl-2 thio hydantoin were synthesized. Their chemical structure was confirmed by IR, NMR and mass spectroscopy. Compounds 1-14 were tested for their anticonvulsant and hypoglycemic activity. Their toxicity was low and they showed only weak activity in tests for anticonvulsive and hypoglycemic properties.     

Synthesis and anticonvulsive activity of some new bisubstituted 1,3,4-oxadiazoles and 1H-1,2,4-triazoles

The synthesis of 7 new 2-[(2-alkoxy-3-methoxyphenyl) methyl]-5-arylamino-1,3,4 oxadiazoles by cyclisation of the corresponding thiosemicarbazides is described. Some of these were tested for anticonvulsant activity. The compound 2-[(2-butoxy-3-methoxy phenyl) methyl]-5-phenylamino 1,3,4-oxadiazole has shown significant anticonvulsant potency. A few new 3-phenyl-5-[(2-alkoxy-3-methoxy phenyl) methyl]-1H-1,2,4 triazoles have also been synthesized.     

Topical mosquito repellents XII: N-substituted ureas and cyclic ureas.

Various N-substituted urea and cyclic urea derivatives were synthesized and evaluated as repellents for Aedes aegypti mosquitoes with an in vitro blood-feeding test system. Several compounds were superior to diethyltoluamide.     

Novel antiepileptic and anticonvulsive therapeutic agents

Epilepsy is a broad-reaching central nervous system condition and the underlying pathology suggests a number of pharmacological pathways that can be targeted for drug therapy. These include ion channel modulation, historically the most investigated therapeutic approach, as well as regulation of excitatory and inhibitory neurotransmission. A broad range of drugs that act at each of these targets has been marketed, and promising new drug candidates are being developed constantly. In addition, new drug candidates with novel mechanisms of action are beginning to emerge. This review covers patent literature with the indication for epilepsy between January 2001 and March 2002, and includes brief overviews and backgrounds on currently used anti-epileptic and anticonvulsive drugs.