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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2001-11-20
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pubmed:abstractText |
Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted beta(3) selectivity. SAR elucidation established that highly selective beta(3) agonists were generated upon substitution of C(alpha) with either benzyl to form (R)-1,2-diarylethylamines or with aryl to generate 1,1-diarylmethylamines. This latter subset yielded a clinical candidate, BMS-194449 (35).(1)
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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 |
Dec
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:Abboa-OffeiB EBE,
pubmed-author:AllenG TGT,
pubmed-author:ArbeenyC MCM,
pubmed-author:CatII,
pubmed-author:ChengPP,
pubmed-author:CiosekC PCPJr,
pubmed-author:DejnekaT CTC,
pubmed-author:DickinsonK EKE,
pubmed-author:FrohlichB HBH,
pubmed-author:GavaiA VAV,
pubmed-author:GeorgeR JRJ,
pubmed-author:GirotraR NRN,
pubmed-author:GreggR ERE,
pubmed-author:HarperT WTW,
pubmed-author:HillyerD EDE,
pubmed-author:MathurAA,
pubmed-author:McCannP JPJ,
pubmed-author:MikkilineniA BAB,
pubmed-author:PossK MKM,
pubmed-author:RoyA CAC,
pubmed-author:RussellA DAD,
pubmed-author:RyonoDD,
pubmed-author:SeymourA AAA,
pubmed-author:SherP MPM,
pubmed-author:SkwishSS,
pubmed-author:SlusarchykD ADA,
pubmed-author:TesfamariamBB,
pubmed-author:WaldronT LTL,
pubmed-author:WangT CTC,
pubmed-author:WashburnW NWN,
pubmed-author:YoungD ADA
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pubmed:issnType |
Print
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pubmed:day |
3
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pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3035-9
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:11714605-Administration, Oral,
pubmed-meshheading:11714605-Adrenergic beta-3 Receptor Agonists,
pubmed-meshheading:11714605-Adrenergic beta-Agonists,
pubmed-meshheading:11714605-Anilides,
pubmed-meshheading:11714605-Animals,
pubmed-meshheading:11714605-Biological Availability,
pubmed-meshheading:11714605-Cercopithecus aethiops,
pubmed-meshheading:11714605-Drug Evaluation, Preclinical,
pubmed-meshheading:11714605-Ethanolamine,
pubmed-meshheading:11714605-Ethanolamines,
pubmed-meshheading:11714605-Humans,
pubmed-meshheading:11714605-Rats,
pubmed-meshheading:11714605-Structure-Activity Relationship
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pubmed:year |
2001
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pubmed:articleTitle |
Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
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pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA. william.washburn@bms.com
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pubmed:publicationType |
Journal Article
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