| pubmed-article:20614888 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20614888 | lifeskim:mentions | umls-concept:C0205145 | lld:lifeskim |
| pubmed-article:20614888 | lifeskim:mentions | umls-concept:C0003286 | lld:lifeskim |
| pubmed-article:20614888 | lifeskim:mentions | umls-concept:C0038477 | lld:lifeskim |
| pubmed-article:20614888 | pubmed:issue | 15 | lld:pubmed |
| pubmed-article:20614888 | pubmed:dateCreated | 2010-8-5 | lld:pubmed |
| pubmed-article:20614888 | pubmed:abstractText | Lacosamide ((R)-N-benzyl 2-acetamido-3-methoxypropionamide, (R)-1) is a low molecular weight anticonvulsant recently introduced in the United States and Europe for adjuvant treatment of partial-onset seizures in adults. In this study, we define the structure-activity relationship (SAR) for the compound's 3-oxy site. Placement of small nonpolar, nonbulky substituents at the 3-oxy site provided compounds with pronounced seizure protection in the maximal electroshock (MES) seizure test with activities similar to (R)-1. The anticonvulsant activity loss that accompanied introduction of larger moieties at the 3-oxy site in (R)-1 was offset, in part, by including unsaturated groups at this position. Our findings were similar to a recently reported SAR study of the 4'-benzylamide site in (R)-1 ( J. Med. Chem. 2010 , 53 , 1288 - 1305 ). Together, these results indicate that both the 3-oxy and 4'-benzylamide positions in (R)-1 can accommodate nonbulky, hydrophobic groups and still retain pronounced anticonvulsant activities in rodents in the MES seizure model. | lld:pubmed |
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| pubmed-article:20614888 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20614888 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20614888 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:20614888 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:20614888 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20614888 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:20614888 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:20614888 | pubmed:author | pubmed-author:StablesJames... | lld:pubmed |
| pubmed-article:20614888 | pubmed:author | pubmed-author:KohnHaroldH | lld:pubmed |
| pubmed-article:20614888 | pubmed:author | pubmed-author:ParkKi DukKD | lld:pubmed |
| pubmed-article:20614888 | pubmed:author | pubmed-author:MorieuxPierre... | lld:pubmed |
| pubmed-article:20614888 | pubmed:author | pubmed-author:SaloméChristo... | lld:pubmed |
| pubmed-article:20614888 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20614888 | pubmed:day | 12 | lld:pubmed |
| pubmed-article:20614888 | pubmed:volume | 53 | lld:pubmed |
| pubmed-article:20614888 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20614888 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20614888 | pubmed:pagination | 5716-26 | lld:pubmed |
| pubmed-article:20614888 | pubmed:dateRevised | 2011-8-15 | lld:pubmed |
| pubmed-article:20614888 | pubmed:meshHeading | pubmed-meshheading:20614888... | lld:pubmed |
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| pubmed-article:20614888 | pubmed:meshHeading | pubmed-meshheading:20614888... | lld:pubmed |
| pubmed-article:20614888 | pubmed:meshHeading | pubmed-meshheading:20614888... | lld:pubmed |
| pubmed-article:20614888 | pubmed:meshHeading | pubmed-meshheading:20614888... | lld:pubmed |
| pubmed-article:20614888 | pubmed:meshHeading | pubmed-meshheading:20614888... | lld:pubmed |
| pubmed-article:20614888 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20614888 | pubmed:articleTitle | The structure-activity relationship of the 3-oxy site in the anticonvulsant (R)-N-benzyl 2-acetamido-3-methoxypropionamide. | lld:pubmed |
| pubmed-article:20614888 | pubmed:affiliation | Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599-7568, USA. | lld:pubmed |
| pubmed-article:20614888 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:20614888 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:20614888 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:20614888 | lld:chembl |
