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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2006-12-25
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pubmed:abstractText |
A novel piperidine series of gamma-secretase inhibitors, potentially useful for the treatment of Alzheimer's disease, is disclosed. SAR investigation revealed the requirement for cis-stereochemistry of the substituents attached to the core, which resulted in the chair-like diaxial conformation of the piperidine ring. The series was optimized to provide inhibitors with IC(50)'s in the single-digit nanomolar range. Absolute stereochemistry of the active enantiomer was assigned.
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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 |
Jan
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AsberomTheodrosT,
pubmed-author:BaraThomas ATA,
pubmed-author:BuevichAlex VAV,
pubmed-author:CladerJohn WJW,
pubmed-author:FuY PYP,
pubmed-author:GreenleeWilliam JWJ,
pubmed-author:GuzikHenry SHS,
pubmed-author:JonesG CGCJr,
pubmed-author:JosienHubert BHB,
pubmed-author:McEwanMichaelM,
pubmed-author:McKittrickBrian ABA,
pubmed-author:NechutaTerry LTL,
pubmed-author:ParkerEric MEM,
pubmed-author:PissarnitskiDmitri ADA,
pubmed-author:SinningLisaL,
pubmed-author:SmithElizabeth MEM,
pubmed-author:VaccaroHenry AHA,
pubmed-author:VoigtJohannes HJH,
pubmed-author:ZhangLiliL,
pubmed-author:ZhangQiQ,
pubmed-author:ZhaoZhiqiangZ
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
57-62
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pubmed:meshHeading |
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pubmed:year |
2007
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pubmed:articleTitle |
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
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pubmed:affiliation |
Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, USA. Dmitri.Pisaarnitski@spcorp.com
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pubmed:publicationType |
Journal Article
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