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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2008-8-11
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pubmed:abstractText |
We describe here a novel 4-amino-2-cyanopyrimidine scaffold for nonpeptidomimetic cathepsin S selective inhibitors. Some of the synthesized compounds have sub-nanomolar potency and high selectivity toward cathepsin S along with promising pharmacokinetic and physicochemical properties. The key structural features of the inhibitors consist of a combination of a spiro[2.5]oct-6-ylmethylamine P2 group at the 4-position, a small or polar P3 group at the 5-position and/or a polar group at the 6-position of the pyrimidine.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:EharaTakeruT,
pubmed-author:GunjiHirokiH,
pubmed-author:HallettAllanA,
pubmed-author:HartTerance WTW,
pubmed-author:HiraoHajimeH,
pubmed-author:HitomiYukoY,
pubmed-author:IrieOsamuO,
pubmed-author:IwakiYukiY,
pubmed-author:IwasakiAtsukoA,
pubmed-author:IwasakiGenjiG,
pubmed-author:KanazawaTakanoriT,
pubmed-author:KishidaMasashiM,
pubmed-author:KonishiKazuhideK,
pubmed-author:KosakaTakatoshiT,
pubmed-author:MasuyaKeiichiK,
pubmed-author:SakakiJunichiJ,
pubmed-author:TanabeKeikoK,
pubmed-author:ToyaoAtsushiA,
pubmed-author:YokokawaFumiakiF
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4642-6
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pubmed:meshHeading |
pubmed-meshheading:18662880-Animals,
pubmed-meshheading:18662880-Cathepsins,
pubmed-meshheading:18662880-Chemistry, Pharmaceutical,
pubmed-meshheading:18662880-Cysteine Proteinase Inhibitors,
pubmed-meshheading:18662880-Drug Design,
pubmed-meshheading:18662880-Humans,
pubmed-meshheading:18662880-Inhibitory Concentration 50,
pubmed-meshheading:18662880-Male,
pubmed-meshheading:18662880-Molecular Conformation,
pubmed-meshheading:18662880-Nitriles,
pubmed-meshheading:18662880-Peptides,
pubmed-meshheading:18662880-Pyrimidines,
pubmed-meshheading:18662880-Rats,
pubmed-meshheading:18662880-Rats, Sprague-Dawley,
pubmed-meshheading:18662880-Recombinant Proteins,
pubmed-meshheading:18662880-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
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pubmed:affiliation |
Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan. osamu.irie@novartis.com
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pubmed:publicationType |
Journal Article
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