| pubmed-article:16759103 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:16759103 | lifeskim:mentions | umls-concept:C0087111 | lld:lifeskim |
| pubmed-article:16759103 | lifeskim:mentions | umls-concept:C0011860 | lld:lifeskim |
| pubmed-article:16759103 | lifeskim:mentions | umls-concept:C0002482 | lld:lifeskim |
| pubmed-article:16759103 | lifeskim:mentions | umls-concept:C1827106 | lld:lifeskim |
| pubmed-article:16759103 | lifeskim:mentions | umls-concept:C2917389 | lld:lifeskim |
| pubmed-article:16759103 | pubmed:issue | 12 | lld:pubmed |
| pubmed-article:16759103 | pubmed:dateCreated | 2006-6-8 | lld:pubmed |
| pubmed-article:16759103 | pubmed:abstractText | A series of beta-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide (6), a potent, orally active DPP-4 inhibitor (IC(50) = 6.3 nM) with excellent selectivity, oral bioavailability in preclinical species, and in vivo efficacy in animal models. Compound 6 was selected for further characterization as a potential new treatment for type 2 diabetes. | lld:pubmed |
| pubmed-article:16759103 | pubmed:language | eng | lld:pubmed |
| pubmed-article:16759103 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16759103 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:16759103 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:16759103 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:Di... | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:ZhuBingB | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:LyonsKathrynK | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:XuShiyaoS | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:ScapinGiovann... | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:MathvinkRober... | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:WeberAnn EAE | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:SmithAaronA | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:ThornberryNan... | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:ShangJackieJ | lld:pubmed |
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| pubmed-article:16759103 | pubmed:author | pubmed-author:EiermannGeorg... | lld:pubmed |
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| pubmed-article:16759103 | pubmed:author | pubmed-author:LeoneJoseph... | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:HarperBartB | lld:pubmed |
| pubmed-article:16759103 | pubmed:author | pubmed-author:LevorseDoroth... | lld:pubmed |
| pubmed-article:16759103 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:16759103 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:16759103 | pubmed:volume | 49 | lld:pubmed |
| pubmed-article:16759103 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:16759103 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:16759103 | pubmed:pagination | 3614-27 | lld:pubmed |
| pubmed-article:16759103 | pubmed:dateRevised | 2011-7-22 | lld:pubmed |
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| pubmed-article:16759103 | pubmed:meshHeading | pubmed-meshheading:16759103... | lld:pubmed |
| pubmed-article:16759103 | pubmed:year | 2006 | lld:pubmed |
| pubmed-article:16759103 | pubmed:articleTitle | (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. | lld:pubmed |
| pubmed-article:16759103 | pubmed:affiliation | Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, New Jersey 07065, USA. scott_edmondson@merck.com | lld:pubmed |
| pubmed-article:16759103 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:16759103 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:16759103 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:16759103 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:16759103 | lld:chembl |
