71 articles for thisTarget
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Article Title
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Synthesis and evaluation of colletoic acid core derivatives.
St. Jude Children'S Research Hospital
Discovery of 11ß-hydroxysteroid dehydrogenase type 1 inhibitor.
Incheon National University
Hupehenols A-E, selective 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors from Viburnum hupehense.
Chinese Academy of Sciences
Synthesis and optimization of picolinamide derivatives as a novel class of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors.
Seoul National University
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Medicinal chemistry of inhibitors of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Astrazeneca
Synthesis of sterically encumbered 11ß-aminoprogesterone derivatives and evaluation as 11ß-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists.
University of Alberta
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11ß-HSD1 inhibitors: potential impact in diabetes.
Chinese Academy of Sciences
Discovery of SAR184841, a potent and long-lasting inhibitor of 11ß-hydroxysteroid dehydrogenase type 1, active in a physiopathological animal model of T2D.
Sanofi R & D
Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors.
Astrazeneca
Novel acidic 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).
Astrazeneca
Optimisation of pharmacokinetic properties in a neutral series of 11ß-HSD1 inhibitors.
Astrazeneca
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11ß-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.
TBA
Discovery of a potent, selective, and orally bioavailable acidic 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).
Astrazeneca
Structure-based design of 7-azaindole-pyrrolidine amides as inhibitors of 11ß-hydroxysteroid dehydrogenase type I.
Merck Serono
Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11ß-hydroxysteroid dehydrogenases.
Chinese Academy of Sciences
Synthesis and evaluation of piperidine urea derivatives as efficacious 11ß-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.
Chinese Academy of Sciences
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Chinese Academy of Sciences
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.
Amgen
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Merck
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
Wyeth Research
Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11ß-hydroxydehydrogenase 1 (11ß-HSD1).
Bristol-Myers Squibb Research & Development
Potent and novel 11ß-HSD1 inhibitors identified from shape and docking based virtual screening.
Shanghai Pharmaceutical Holding
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.
Vitae Pharmaceuticals
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Substituted phenyl triazoles as selective inhibitors of 11 β-Hydroxysteroid Dehydrogenase Type 1.
Merck
Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.
Sanofi-Aventis R&D
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.
Merck Research Laboratories
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11ß-hydroxysteroid dehydrogenase 2 inhibitors.
University of Technology
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Vitae Pharmaceuticals
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11ß-hydroxysteroid dehydrogenase 2 inhibitors.
University of Natural Resources and Applied Life Sciences
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Amgen
Synthesis of glycyrrhetinic acid derivatives for the treatment of metabolic diseases.
Vienna University of Technology
Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.
Vitae Pharmaceuticals
Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Serono
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
TBA
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Amgen
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Biovitrum
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Abbott Laboratories
Progress in 11β-HSD1 inhibitors for the treatment of metabolic diseases: A comprehensive guide to their chemical structure diversity in drug development.
Hong Kong Baptist University
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
Abbott Laboratories
Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.
Abbott Laboratories
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.
Abbott Laboratories
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Abbott Laboratories
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
University of Innsbruck
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Merck
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.
Incyte Research Institute
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Wyeth Research
A novel 18 beta-glycyrrhetinic acid analogue as a potent and selective inhibitor of 11 beta-hydroxysteroid dehydrogenase 2.
University of Bath
Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1).
Sk Chemicals
Mechanistic Insight on the Mode of Action of Colletoic Acid.
The University of Tennessee Health Science Center
Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction.
Universitat De Barcelona
Synthesis of selective 11β-HSD1 inhibitors based on dammarane scaffold.
Chinese Academy of Sciences
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.
Vitae Pharmaceuticals
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.
Bristol-Myers Squibb
COMPOSITIONS AND METHODS FOR TREATING, PREVENTING OR REVERSING AGE-ASSOCIATED INFLAMMATION AND DISORDER
Brown University
SUBSTITUTED PYRROLO [2, 3-b] PYRIDINE AND PYRAZOLO [3, 4-b] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
Fochon Biosciences
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Saarland University