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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2008-5-5
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pubmed:abstractText |
N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives 1-8 were synthesized and evaluated for their in vivo antidiabetic activity in a non-insulin-dependent diabetes mellitus rat model. Several compounds synthesized showed significant lowering of plasma glucose level in this model. As a possible mode of action, the compounds were in vitro evaluated as 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors. The most active compounds (3 and 4) were docked into the crystal structure of 11beta-HSD1. Docking results indicate potential hydrogen bond interactions with catalytic amino acid residues.
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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 |
May
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BinnieMargaretM,
pubmed-author:Díaz-CoutiñoDanielD,
pubmed-author:Estrada-SotoSamuelS,
pubmed-author:Ibarra-BarajasMaximilianoM,
pubmed-author:León-RiveraIsmaelI,
pubmed-author:Medina-FrancoJose LuisJL,
pubmed-author:Moreno-DíazHermenegildaH,
pubmed-author:Navarrete-VázquezGabrielG,
pubmed-author:Ortiz-AndradeRolffyR,
pubmed-author:Villalobos-MolinaRafaelR,
pubmed-author:WebsterScott PSP
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2871-7
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pubmed:meshHeading |
pubmed-meshheading:18424136-11-beta-Hydroxysteroid Dehydrogenase Type 1,
pubmed-meshheading:18424136-Amino Acid Sequence,
pubmed-meshheading:18424136-Binding Sites,
pubmed-meshheading:18424136-Blood Glucose,
pubmed-meshheading:18424136-Cell Line,
pubmed-meshheading:18424136-Enzyme Inhibitors,
pubmed-meshheading:18424136-Humans,
pubmed-meshheading:18424136-Hydrogen Bonding,
pubmed-meshheading:18424136-Hypoglycemic Agents,
pubmed-meshheading:18424136-Kidney,
pubmed-meshheading:18424136-Models, Chemical,
pubmed-meshheading:18424136-Molecular Sequence Data,
pubmed-meshheading:18424136-Structure-Activity Relationship,
pubmed-meshheading:18424136-Sulfonamides
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pubmed:year |
2008
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pubmed:articleTitle |
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides.
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pubmed:affiliation |
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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