75 articles for thisTarget
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Article Title
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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
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Seoul National University
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
Chinese Academy of Sciences
Lithocarpic acids O-S, five homo-cycloartane derivatives from the cupules of Lithocarpus polystachyus.
TBA
Ingol-type diterpenes from Euphorbia antiquorum with mouse 11ß-hydroxysteroid dehydrogenase type 1 inhibition activity.
Lanzhou University
Medicinal chemistry of inhibitors of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Astrazeneca
Optimization of brain penetrant 11ß-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.
Astrazeneca
3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11ß-hydroxysteroid dehydrogenase 1 inhibitor.
Yonsei University
Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Bristol-Myers Squibb
1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11ß-HSD1 inhibitors for the treatment of diabetes.
Sanofi Deutschland
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
Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1.
Toray Industries
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 biological evaluation of cyclic sulfamide derivatives as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
TBA
Synthesis and evaluation of piperidine urea derivatives as efficacious 11ß-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.
Chinese Academy of Sciences
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
TBA
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 dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
Chinese Academy of Sciences
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
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.
Shanghai Institute of Materia Medica
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
Biovitrum
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
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1).
Bristol-Myers Squibb
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 and 11ß hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.
Korea University
Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors.
Korea University
The discovery of azepane sulfonamides as potent 11beta-HSD1 inhibitors.
Schering-Plough Research Institute
Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model.
Wyeth Research
Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Serono
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
Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors.
Institute of Materia Medica
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
Wyeth Research
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors.
University of Edinburgh
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
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 11?-HSD1 using a scaffold-hopping approach.
Incyte Research Institute
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 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD1).
Sk Chemicals
Optimization of cyclic sulfamide derivatives as 11?-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.
Korea Research Institute of Chemical Technology
Limonoids and Triterpenoids as 11?-HSD1 Inhibitors from Walsura robusta.
Chinese Academy of Sciences
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD-1).
Bristol-Myers Squibb
Design, synthesis and in vivo study of novel pyrrolidine-based 11?-HSD1 inhibitors for age-related cognitive dysfunction.
Universitat De Barcelona
Synthesis of selective 11?-HSD1 inhibitors based on dammarane scaffold.
Chinese Academy of Sciences
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 11?-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.
Bristol-Myers Squibb
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Merck Frosst Centre For Therapeutic Research
Design and synthesis of conformationally constrained cyclophilin inhibitors showing a cyclosporin-A phenotype in C. elegans.
The University of Edinburgh