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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2005-5-31
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pubmed:abstractText |
anti-Substituted biaryl beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors that suffer from suboptimal selectivity and pharmacokinetics. This letter describes the substitution of the beta-methyl substituent with beta-polar substituents, culminating in the discovery of a beta-dimethylamide substituted phenylalanine derivative with an excellent potency, selectivity, and pharmacokinetic profile.
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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 |
Jun
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AliT ZTZ,
pubmed-author:DuffyJoseph LJL,
pubmed-author:EdmondsonScott DSD,
pubmed-author:EiermannGeorge JGJ,
pubmed-author:HeHuaibingH,
pubmed-author:LeitingBarbaraB,
pubmed-author:LeoneJoseph FJF,
pubmed-author:LyonsKathryn AKA,
pubmed-author:MakarewiczAmanda MAM,
pubmed-author:MastracchioAnthonyA,
pubmed-author:PatelReshma ARA,
pubmed-author:PetrovAleksandrA,
pubmed-author:ThornberryNancy ANA,
pubmed-author:WeberAnn EAE,
pubmed-author:WuJoseph KJK
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3048-52
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:15908206-Administration, Oral,
pubmed-meshheading:15908206-Animals,
pubmed-meshheading:15908206-Blood Glucose,
pubmed-meshheading:15908206-DNA-Binding Proteins,
pubmed-meshheading:15908206-Dipeptidyl Peptidase 4,
pubmed-meshheading:15908206-Glucose Tolerance Test,
pubmed-meshheading:15908206-Humans,
pubmed-meshheading:15908206-Mice,
pubmed-meshheading:15908206-Molecular Structure,
pubmed-meshheading:15908206-Phenylalanine,
pubmed-meshheading:15908206-Protease Inhibitors,
pubmed-meshheading:15908206-Rats,
pubmed-meshheading:15908206-Structure-Activity Relationship,
pubmed-meshheading:15908206-Substrate Specificity,
pubmed-meshheading:15908206-Trans-Activators
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pubmed:year |
2005
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pubmed:articleTitle |
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. scott_edmondson@merck.com
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pubmed:publicationType |
Journal Article
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