145 articles for thisTarget
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Synthesis and evaluation of colletoic acid core derivatives.
St. Jude Children'S Research Hospital
Novel 11ß-HSD1 inhibitors: C-1 versus C-2 substitution and effect of the introduction of an oxygen atom in the adamantane scaffold.
Universitat De Barcelona
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
Ligand-based pharmacophore modeling and virtual screening for the discovery of novel 17ß-hydroxysteroid dehydrogenase 2 inhibitors.
University of Innsbruck
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
Discovery of pyridyl sulfonamide 11-beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors for the treatment of metabolic disorders.
Bristol-Myers Squibb
Ingol-type diterpenes from Euphorbia antiquorum with mouse 11ß-hydroxysteroid dehydrogenase type 1 inhibition activity.
Lanzhou University
Discovery of camphor-derived pyrazolones as 11ß-hydroxysteroid dehydrogenase type 1 inhibitors.
Hoffmann-La Roche
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
Synthesis of sterically encumbered 11ß-aminoprogesterone derivatives and evaluation as 11ß-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists.
University of Alberta
Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Leopold-Franzens-Universit£T
1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11ß-HSD1 inhibitors for the treatment of diabetes.
Sanofi Deutschland
Mono-carbonyl curcumin analogues as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Wenzhou Medical College
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
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11ß-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.
Pfizer
Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1.
Toray Industries
Design, synthesis and SAR of piperidyl-oxadiazoles as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Chinese Academy of Sciences
Structural optimization of 2,5-thiophene amides as highly potent and selective 17ß-hydroxysteroid dehydrogenase type 2 inhibitors for the treatment of osteoporosis.
Saarland University
Docking-based 3D-QSAR study for 11beta-HSD1 inhibitors.
Korea Research Institute of Chemical Technology
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
Adamantyl carboxamides and acetamides as potent human 11ß-hydroxysteroid dehydrogenase type 1 inhibitors.
University of Bath
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
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11ß-HSD1 inhibitors.
Amgen
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
Synthesis and biological evaluation of (6- and 7-phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17ß-hydroxysteroid dehydrogenase type 1.
University of Ljubljana
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
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
Amgen
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
Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries.
University of Innsbruck
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
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
Wyeth Research
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
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
Synthesis and 11ß hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.
Korea University
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11ß-HSD1 inhibitors.
Amgen
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
A statistical analysis of in vitro human microsomal metabolic stability of small phenyl group substituents, leading to improved design sets for parallel SAR exploration of a chemical series.
Astrazeneca
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
Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
University of Edinburgh
Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors.
Korea University
Synthesis of glycyrrhetinic acid derivatives for the treatment of metabolic diseases.
Vienna University of Technology
11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches.
University of Innsbruck
Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.
Vitae Pharmaceuticals
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
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
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
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
Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Biovitrum
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
Designing Out PXR Activity on Drug Discovery Projects: A Review of Structure-Based Methods, Empirical and Computational Approaches.
Ucb
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
Dammarane-type leads panaxadiol and protopanaxadiol for drug discovery: Biological activity and structural modification.
Shenyang Pharmaceutical 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 subgroup of 2'-hydroxy-flavonoids: Molecular diversity, mechanism of action, and anticancer properties.
Oncowitan
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
Discovery of a novel 2-spiroproline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.
Incyte Research Institute
Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells.
University of Manchester
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
Optimization of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.
Korea Research Institute of Chemical Technology
Limonoids and Triterpenoids as 11β-HSD1 Inhibitors from Walsura robusta.
Chinese Academy of Sciences
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
Bristol-Myers Squibb
Mechanistic Insight on the Mode of Action of Colletoic Acid.
The University of Tennessee Health Science Center
Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors.
Universitat De Barcelona
Accelerated skin wound healing by selective 11β-Hydroxylase (CYP11B1) inhibitors.
Saarland University
Design, synthesis, and biological evaluation of novel selective peptide inhibitors of 11β-hydroxysteroid dehydrogenase 1.
Dsm Nutritional Products
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
Orvinol and thevinol derivatives useful in the treatment of depression
The University of Bath
Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
Nerviano Medical Sciences
Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin.
Nih
Biological evaluation and structural determinants of p38α mitogen-activated-protein kinase and c-Jun-N-terminal kinase 3 inhibition by flavonoids.
Eberhard Karls University of Tuebingen
Effects of remoxipride and some related new substituted salicylamides on rat brain receptors.
Astra LÄKemedel
Selective alpha-2 adrenoceptor blockade by SK&F 86466: in vitro characterization of receptor selectivity.
Smith Kline & French Laboratories
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Astrazeneca
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.
National Taiwan University
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Saarland University