| pubmed-article:20122828 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C0006104 | lld:lifeskim |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C0268563 | lld:lifeskim |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C1412727 | lld:lifeskim |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C1441547 | lld:lifeskim |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C0439831 | lld:lifeskim |
| pubmed-article:20122828 | lifeskim:mentions | umls-concept:C0205372 | lld:lifeskim |
| pubmed-article:20122828 | pubmed:issue | 5 | lld:pubmed |
| pubmed-article:20122828 | pubmed:dateCreated | 2010-2-22 | lld:pubmed |
| pubmed-article:20122828 | pubmed:abstractText | This Letter describes the one pot synthesis of tertiary carbinamine 3 and related analogs of brain penetrant BACE-1 inhibitors via the alkylation of the Schiff base intermediate 2. The methodology developed for this study provided a convenient and rapid means to explore the P1 region of these types of inhibitors, where the P1 group is installed in the final step using a one-pot two-step protocol. Further SAR studies led to the identification of 10 which is twofold more potent in vitro as compared to the lead compound. This inhibitor was characterized in a cisterna magna ported rhesus monkey model, where significant lowering of CSF Abeta40 was observed. | lld:pubmed |
| pubmed-article:20122828 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20122828 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20122828 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20122828 | pubmed:month | Mar | lld:pubmed |
| pubmed-article:20122828 | pubmed:issn | 1464-3405 | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:ZhuHongH | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:NantermetPhil... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:HazudaDaria... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:ColussiDennis... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:GrahamSamuel... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:SimonAdamA | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:RajapakseHema... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:LaiMing-TainM... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:VaccaJoseph... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:HolahanMarie... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:CookJacquelyn... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:ShiXiao-PingX... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:TugushevaKath... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:PriceEric AEA | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:Sankaranaraya... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:PietrakBethB | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:MichenerMaria... | lld:pubmed |
| pubmed-article:20122828 | pubmed:author | pubmed-author:YoungMary BMB | lld:pubmed |
| pubmed-article:20122828 | pubmed:copyrightInfo | Copyright 2010 Elsevier Ltd. All rights reserved. | lld:pubmed |
| pubmed-article:20122828 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20122828 | pubmed:day | 1 | lld:pubmed |
| pubmed-article:20122828 | pubmed:volume | 20 | lld:pubmed |
| pubmed-article:20122828 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20122828 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20122828 | pubmed:pagination | 1779-82 | lld:pubmed |
| pubmed-article:20122828 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:meshHeading | pubmed-meshheading:20122828... | lld:pubmed |
| pubmed-article:20122828 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20122828 | pubmed:articleTitle | Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors. | lld:pubmed |
| pubmed-article:20122828 | pubmed:affiliation | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. | lld:pubmed |
| pubmed-article:20122828 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:20122828 | lld:chembl |
