| pubmed-article:12824035 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C0023621 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C0040048 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C1413665 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C0015505 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C2348042 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C0048701 | lld:lifeskim |
| pubmed-article:12824035 | lifeskim:mentions | umls-concept:C1434724 | lld:lifeskim |
| pubmed-article:12824035 | pubmed:issue | 14 | lld:pubmed |
| pubmed-article:12824035 | pubmed:dateCreated | 2003-6-25 | lld:pubmed |
| pubmed-article:12824035 | pubmed:abstractText | A solution-phase synthesis of an alpha-ketothiazole library of the general form D-Phe-L-AA-L-Arg-alpha-ketothiazole is described. The five-step synthesis is accomplished using a combination of polymeric reagents and polymer-assisted solution-phase purification protocols, including reactant-sequestering resins, reagent-sequestering resins, and tagged reagents. The multi-step synthesis affords the desired alpha-ketothiazole products in excellent purities and yields. A variety of L-amino acid inputs were used to probe the S2 pocket of the tissue factor (TF) VIIa enzyme to influence both potency and selectivity. An X-ray crystal structure of compound 10e bound to the TF/VIIa complex was obtained that explains the observed selectivity. The alpha-ketothiazoles were found to be potent, reversible-covalent inhibitors of tissue factor VIIa, with some analogues demonstrating selectivity versus thrombin. | lld:pubmed |
| pubmed-article:12824035 | pubmed:language | eng | lld:pubmed |
| pubmed-article:12824035 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:12824035 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12824035 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12824035 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:12824035 | pubmed:issn | 0960-894X | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:StallingsWill... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:StevensAnna... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:KurumbailRavi... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:GirardThomas... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:SouthMichael... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:LachanceRhond... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:StegemanRoder... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:ParlowJohn... | lld:pubmed |
| pubmed-article:12824035 | pubmed:author | pubmed-author:DiceThomas... | lld:pubmed |
| pubmed-article:12824035 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12824035 | pubmed:day | 21 | lld:pubmed |
| pubmed-article:12824035 | pubmed:volume | 13 | lld:pubmed |
| pubmed-article:12824035 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12824035 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12824035 | pubmed:pagination | 2363-7 | lld:pubmed |
| pubmed-article:12824035 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:meshHeading | pubmed-meshheading:12824035... | lld:pubmed |
| pubmed-article:12824035 | pubmed:year | 2003 | lld:pubmed |
| pubmed-article:12824035 | pubmed:articleTitle | Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors. | lld:pubmed |
| pubmed-article:12824035 | pubmed:affiliation | Department of Medicinal and Combinatorial Chemistry, Pharmacia Corporation, 800 North Lindbergh Boulevard, 63167, St. Louis, MO, USA. michael.s.south@pharmacia.com | lld:pubmed |
| pubmed-article:12824035 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:12824035 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:12824035 | lld:chembl |
