The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
26820555 |
87 |
Synthesis and evaluation of colletoic acid core derivatives. |
St. Jude Children'S Research Hospital |
26306982 |
4 |
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 |
26187704 |
63 |
Discovery of 11ß-hydroxysteroid dehydrogenase type 1 inhibitor. |
Incheon National University |
25590374 |
23 |
Hupehenols A-E, selective 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors from Viburnum hupehense. |
Chinese Academy of Sciences |
25800116 |
62 |
Synthesis and optimization of picolinamide derivatives as a novel class of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors. |
Seoul National University |
25529735 |
27 |
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1). |
Seoul National University |
25050169 |
52 |
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1). |
Bristol-Myers Squibb |
24960438 |
24 |
Ligand-based pharmacophore modeling and virtual screening for the discovery of novel 17ß-hydroxysteroid dehydrogenase 2 inhibitors. |
University of Innsbruck |
25098388 |
7 |
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus. |
Chinese Academy of Sciences |
25453795 |
6 |
Lithocarpic acids O-S, five homo-cycloartane derivatives from the cupules of Lithocarpus polystachyus. |
TBA |
25266782 |
41 |
Discovery of pyridyl sulfonamide 11-beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors for the treatment of metabolic disorders. |
Bristol-Myers Squibb |
24815509 |
51 |
Discovery of camphor-derived pyrazolones as 11ß-hydroxysteroid dehydrogenase type 1 inhibitors. |
Hoffmann-La Roche |
24294985 |
42 |
Medicinal chemistry of inhibitors of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1). |
Astrazeneca |
24422550 |
107 |
Optimization of brain penetrant 11ß-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice. |
Astrazeneca |
24507919 |
45 |
3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11ß-hydroxysteroid dehydrogenase 1 inhibitor. |
Yonsei University |
24360604 |
60 |
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 |
24074876 |
17 |
Synthesis of sterically encumbered 11ß-aminoprogesterone derivatives and evaluation as 11ß-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists. |
University of Alberta |
23981897 |
6 |
Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11ß-hydroxysteroid dehydrogenase 1 inhibitors. |
Leopold-Franzens-Universit£T |
23845218 |
86 |
1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11ß-HSD1 inhibitors for the treatment of diabetes. |
Sanofi Deutschland |
23795939 |
5 |
11ß-HSD1 inhibitors from Walsura cochinchinensis. |
Chinese Academy of Sciences |
23800686 |
45 |
Mono-carbonyl curcumin analogues as 11ß-hydroxysteroid dehydrogenase 1 inhibitors. |
Wenzhou Medical College |
23747808 |
51 |
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11ß-HSD1 inhibitors: potential impact in diabetes. |
Chinese Academy of Sciences |
23659858 |
17 |
Evaluation of selective inhibitors of 11ß-HSD1 for the treatment of hypertension. |
Merck |
23478147 |
42 |
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 |
23489629 |
19 |
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11ß-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
Pfizer |
23414800 |
47 |
Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1. |
Toray Industries |
23353742 |
29 |
Design, synthesis and SAR of piperidyl-oxadiazoles as 11ß-hydroxysteroid dehydrogenase 1 inhibitors. |
Chinese Academy of Sciences |
23145773 |
45 |
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 |
24900572 |
54 |
Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes. |
Pfizer |
18314331 |
70 |
Docking-based 3D-QSAR study for 11beta-HSD1 inhibitors. |
Korea Research Institute of Chemical Technology |
23153367 |
92 |
Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors. |
Astrazeneca |
23088558 |
36 |
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 |
23040895 |
37 |
Adamantyl carboxamides and acetamides as potent human 11ß-hydroxysteroid dehydrogenase type 1 inhibitors. |
University of Bath |
23013933 |
59 |
Optimisation of pharmacokinetic properties in a neutral series of 11ß-HSD1 inhibitors. |
Astrazeneca |
24900382 |
41 |
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11ß-Hydroxysteroid Dehydrogenase Type 1 Inhibitors. |
TBA |
22691057 |
32 |
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 |
22901389 |
28 |
Structure-based design of 7-azaindole-pyrrolidine amides as inhibitors of 11ß-hydroxysteroid dehydrogenase type I. |
Merck Serono |
22542009 |
102 |
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11ß-HSD1 inhibitors. |
Amgen |
22360639 |
12 |
Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11ß-hydroxysteroid dehydrogenases. |
Chinese Academy of Sciences |
24900439 |
34 |
Synthesis and biological evaluation of cyclic sulfamide derivatives as 11ß-hydroxysteroid dehydrogenase 1 inhibitors. |
TBA |
22440625 |
44 |
Synthesis and evaluation of piperidine urea derivatives as efficacious 11ß-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice. |
Chinese Academy of Sciences |
24900270 |
22 |
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
TBA |
21138273 |
11 |
Synthesis and biological evaluation of (6- and 7-phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17ß-hydroxysteroid dehydrogenase type 1. |
University of Ljubljana |
19564108 |
48 |
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 |
19574056 |
25 |
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes. |
Chinese Academy of Sciences |
19185488 |
56 |
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors. |
Amgen |
18553955 |
43 |
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 |
18533708 |
25 |
Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries. |
University of Innsbruck |
18440812 |
113 |
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
Merck Research Laboratories |
18434143 |
96 |
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. |
Merck |
18242087 |
18 |
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling. |
Shanghai Institute of Materia Medica |
17490884 |
39 |
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action. |
Wyeth Research |
12190302 |
9 |
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. |
Biovitrum |
22148241 |
3 |
Cyclopeptide Alkaloids from Ziziphus apetala. |
Kunming Institute of Botany |
21983444 |
78 |
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 |
21983439 |
65 |
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 |
21873057 |
13 |
Potent and novel 11ß-HSD1 inhibitors identified from shape and docking based virtual screening. |
Shanghai Pharmaceutical Holding |
21786805 |
130 |
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1. |
Vitae Pharmaceuticals |
21689935 |
55 |
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 |
21334894 |
218 |
Substituted phenyl triazoles as selective inhibitors of 11 β-Hydroxysteroid Dehydrogenase Type 1. |
Merck |
21439819 |
49 |
Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1. |
Sanofi-Aventis R&D |
21421311 |
135 |
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome. |
Merck Research Laboratories |
21376605 |
26 |
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 |
21093259 |
38 |
Synthesis and 11ß hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group. |
Korea University |
21093258 |
66 |
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11ß-HSD1 inhibitors. |
Amgen |
20971000 |
76 |
The synthesis and SAR of novel diarylsulfone 11ß-HSD1 inhibitors. |
Amgen |
20864344 |
110 |
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1. |
Vitae Pharmaceuticals |
20851614 |
22 |
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 |
20510621 |
44 |
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 |
20465278 |
27 |
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 |
20452767 |
65 |
Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles. |
University of Edinburgh |
20363126 |
50 |
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
Pfizer |
20149650 |
65 |
Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors. |
Merck Research Laboratories |
20045318 |
18 |
Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors. |
Korea University |
20100662 |
6 |
11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches. |
University of Innsbruck |
20064717 |
64 |
Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design. |
Vitae Pharmaceuticals |
19625185 |
44 |
The discovery of azepane sulfonamides as potent 11beta-HSD1 inhibitors. |
Schering-Plough Research Institute |
19673466 |
101 |
Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model. |
Wyeth Research |
19395260 |
29 |
Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
Merck Serono |
19181519 |
71 |
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). |
TBA |
19053753 |
67 |
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 |
18789704 |
4 |
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. |
Amgen |
18653260 |
24 |
Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors. |
Institute of Materia Medica |
18578516 |
83 |
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 |
18440811 |
207 |
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
Merck Research Laboratories |
17919905 |
56 |
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. |
Amgen |
17600707 |
48 |
Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. |
Biovitrum |
17442567 |
27 |
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors. |
Biovitrum |
17350260 |
56 |
Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors. |
University of Edinburgh |
17201418 |
105 |
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors. |
Abbott Laboratories |
17070044 |
102 |
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors. |
Abbott Laboratories |
17000111 |
127 |
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome. |
Abbott Laboratories |
16996734 |
93 |
Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction. |
Abbott Laboratories |
16931002 |
73 |
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors. |
Abbott Laboratories |
16899366 |
85 |
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors. |
Abbott Laboratories |
16890427 |
81 |
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements. |
Abbott Laboratories |
16759088 |
38 |
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening. |
University of Innsbruck |
16185866 |
53 |
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 |
15911270 |
19 |
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
Wyeth Research |
31759849 |
24 |
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 |
26936592 |
8 |
Limonoids and Triterpenoids as 11?-HSD1 Inhibitors from Walsura robusta. |
Chinese Academy of Sciences |
30613321 |
31 |
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD-1). |
Bristol-Myers Squibb |
31294974 |
62 |
Mechanistic Insight on the Mode of Action of Colletoic Acid. |
The University of Tennessee Health Science Center |
26596711 |
3 |
Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11?-HSD1 inhibitors. |
Universitat De Barcelona |
29207342 |
7 |
Accelerated skin wound healing by selective 11?-Hydroxylase (CYP11B1) inhibitors. |
Saarland University |
30245006 |
5 |
Design, synthesis, and biological evaluation of novel selective peptide inhibitors of 11?-hydroxysteroid dehydrogenase 1. |
Dsm Nutritional Products |
28818766 |
23 |
Design, synthesis and in vivo study of novel pyrrolidine-based 11?-HSD1 inhibitors for age-related cognitive dysfunction. |
Universitat De Barcelona |
28458137 |
25 |
Synthesis of selective 11?-HSD1 inhibitors based on dammarane scaffold. |
Chinese Academy of Sciences |
28528082 |
140 |
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11? hydroxysteroid dehydrogenase type 1 inhibitor. |
Vitae Pharmaceuticals |
28537398 |
114 |
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 |
22145694 |
64 |
Simple methanesulfonates are hydrolyzed by the sulfatase carbonic anhydrase activity. |
Agri Ibrahim Cecen University |
20233015 |
6 |
Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukesová 27/97. |
Brno University of Technology |
28460360 |
13 |
Design, synthesis and biological activity of 3-oxoamino-benzenesulfonamides as selective and reversible LSD1 inhibitors. |
China Pharmaceutical University |
27982494 |
6 |
Polar Hinges as Functionalized Conformational Constraints in (Bi)cyclic Peptides. |
University of Glasgow |
21538764 |
6 |
Identification and characterization of new inhibitors of fungal homoserine kinase. |
Mcmaster University |
21337480 |
17 |
Design and synthesis of conformationally constrained cyclophilin inhibitors showing a cyclosporin-A phenotype in C. elegans. |
The University of Edinburgh |
8097160 |
35 |
Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective. |
University of Toronto |
20187655 |
12 |
Development of GlcNAc-inspired iminocyclitiols as potent and selective N-acetyl-beta-hexosaminidase inhibitors. |
Academia Sinica |
19807124 |
8 |
Chemical library screens targeting an HIV-1 accessory factor/host cell kinase complex identify novel antiretroviral compounds. |
University of Pittsburgh |
19438227 |
71 |
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors. |
Pfizer |