McComsey, David F. published the artcileNovel, Broad-Spectrum Anticonvulsants Containing a Sulfamide Group: Pharmacological Properties of (S)-N-[(6-Chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112), Quality Control of 115314-17-5, the publication is Journal of Medicinal Chemistry (2013), 56(22), 9019-9030, database is CAplus and MEDLINE.
Broad-spectrum anticonvulsants are of considerable interest as antiepileptic drugs, especially because of their potential for treating refractory patients. Such “neurostabilizers” have also been used to treat other neurol. disorders, including migraine, bipolar disorder, and neuropathic pain. A series of sulfamide derivatives was synthesized and their anticonvulsant activity evaluted. Thus, the authors identified promising sulfamide I (JNJ-26489112) and explored its pharmacol. properties. Compound I exhibited excellent anticonvulsant activity in rodents against audiogenic, elec. induced, and chem. induced seizures. Mechanistically, I inhibited voltage-gated Na+ channels and N-type Ca2+ channels and was effective as a K+ channel opener. The anticonvulsant profile of I suggests that it may be useful for treating multiple forms of epilepsy (generalized tonic-clonic, complex partial, absence seizures), including refractory (or pharmacoresistant) epilepsy, at dose levels that confer a good safety margin. On the basis of its pharmacol. and other favorable characteristics, I was advanced into human clin. studies.
Journal of Medicinal Chemistry published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Quality Control of 115314-17-5.
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