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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2010-8-16
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pubmed:abstractText |
SAR studies to improve the selectivity and metabolic stability of a class of recently discovered MMP-13 inhibitors are reported. Improved selectivity was achieved by modifying interactions with the S1' pocket. Metabolic stability was improved through reduction of inhibitor lipophilicity. This translated into lower in vivo clearance for the preferred compound.
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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 |
Sep
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AmodeoLauraL,
pubmed-author:AugustE MichaelEM,
pubmed-author:CaoXianhuaX,
pubmed-author:CiccarelliLeonardL,
pubmed-author:CollinsBrandon KBK,
pubmed-author:FarrowNeil ANA,
pubmed-author:GaoDonghong AmyDA,
pubmed-author:HarringtonKyleK,
pubmed-author:HavertyKathleenK,
pubmed-author:Heim-RietherAlexanderA,
pubmed-author:Hill-DrzewiMelissaM,
pubmed-author:KeenanLana SmithLS,
pubmed-author:LiXiangX,
pubmed-author:LiangShuangS,
pubmed-author:MargaritSteluta MarianaSM,
pubmed-author:MeeSS,
pubmed-author:MossNeilN,
pubmed-author:NagarajaNelamangalaN,
pubmed-author:ProudfootJohnJ,
pubmed-author:RomanReneR,
pubmed-author:SchlyerSabineS,
pubmed-author:TaylorStevenS,
pubmed-author:WellenzohnBerndB,
pubmed-author:WiedenmayerDieterD,
pubmed-author:XiongZhaomingZ
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5039-43
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability.
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pubmed:affiliation |
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877, USA. amy.gao@boehringer-ingelheim.com
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pubmed:publicationType |
Journal Article
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