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Review

11β-Hydroxysteroid dehydrogenase type 1 inhibitors as therapeutic agents

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Pages 1407-1422 | Published online: 06 Dec 2007

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (3)

Alex Odermatt. (2009) Diazepane–acetamide derivatives as selective 11β-hydroxysteroid dehydrogenase type 1 inhibitors. Expert Opinion on Therapeutic Patents 19:10, pages 1477-1483.
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Craig D Boyle & Timothy J Kowalski. (2009) 11β-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents. Expert Opinion on Therapeutic Patents 19:6, pages 801-825.
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Katherine A Hughes, Scott P Webster & Brian R Walker. (2008) 11-Beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in Type 2 diabetes mellitus and obesity. Expert Opinion on Investigational Drugs 17:4, pages 481-496.
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Articles from other publishers (33)

Danyang Zhang, Dan Xu, Xinyue Chen, Huan Zhou & Gong Xu. (2021) Divergent Entry to Walsucochin Nortriterpenoids: Total Syntheses of (±)-Walsucochin A and (±)-Walsucochinoids C–F. The Journal of Organic Chemistry 86:10, pages 7271-7279.
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博 李. (2018) Progress in Hypoglycemic and Lipid-Lowering Drugs. Journal of Comparative Chemistry 02:04, pages 142-160.
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Elena Valverde, Constantí Seira, Andrew McBride, Margaret Binnie, F. Javier Luque, Scott P. Webster, Axel Bidon-Chanal & Santiago Vázquez. (2015) Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors. Bioorganic & Medicinal Chemistry 23:24, pages 7607-7617.
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Steven Shave, Elizabeth A. Blackburn, Jillian Adie, Douglas R. Houston, Manfred Auer, Scott P. Webster, Paul Taylor & Malcolm D. Walkinshaw. (2015) UFSRAT: Ultra-Fast Shape Recognition with Atom Types –The Discovery of Novel Bioactive Small Molecular Scaffolds for FKBP12 and 11βHSD1. PLOS ONE 10:2, pages e0116570.
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Graeme R. Robb, Scott Boyd, Christopher D. Davies, Alexander G. Dossetter, Frederick W. Goldberg, Paul D. Kemmitt, James S. Scott & John G. Swales. (2015) Design of pyrazolo-pyrimidines as 11β-HSD1 inhibitors through optimisation of molecular electrostatic potential. MedChemComm 6:5, pages 926-934.
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James S. ScottFrederick W. GoldbergAndrew V. Turnbull. (2013) Medicinal Chemistry of Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). Journal of Medicinal Chemistry 57:11, pages 4466-4486.
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Gabriel Navarrete-Vázquez, Maria Guadalupe Morales-Vilchis, Samuel Estrada-Soto, Juan José Ramírez-Espinosa, Sergio Hidalgo-Figueroa, Carlos Nava-Zuazo, Hugo Tlahuext, Ismael Leon-Rivera, José L. Medina-Franco, Fabian López-Vallejo, Scott P. Webster, Margaret Binnie, Rolffy Ortiz-Andrade & Hermenegilda Moreno-Diaz. (2014) Synthesis of 2-{2-[(α/β-naphthalen-1-ylsulfonyl)amino]-1,3-thiazol-4-yl} acetamides with 11β-hydroxysteroid dehydrogenase inhibition and in combo antidiabetic activities. European Journal of Medicinal Chemistry 74, pages 179-186.
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Jin-Hai Yu, Yu Shen, Hong-Bing Liu, Ying Leng, Hua Zhang & Jian-Min Yue. (2014) Dammarane-type triterpenoids as 11β-HSD1 inhibitors from Homonoia riparia. Org. Biomol. Chem. 12:26, pages 4716-4722.
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William McCoull, Martin Augustin, Caroline Blake, Anne Ertan, Elaine Kilgour, Stephan Krapp, Jane E. Moore, Nicholas J. Newcombe, Martin J. Packer, Amanda Rees, John Revill, James S. Scott, Nidhal Selmi, Stefan Gerhardt, Derek J. Ogg, Stefan Steinbacher & Paul R. O. Whittamore. (2014) Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). Med. Chem. Commun. 5:1, pages 57-63.
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Anna Anderson & Brian R. Walker. (2013) 11β-HSD1 Inhibitors for the Treatment of Type 2 Diabetes and Cardiovascular Disease. Drugs 73:13, pages 1385-1393.
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Mei-Ling Han, Yu Shen, Guo-Cai Wang, Ying Leng, Hua Zhang & Jian-Min Yue. (2013) 11β-HSD1 Inhibitors from Walsura cochinchinensis . Journal of Natural Products 76:7, pages 1319-1327.
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Patrick W. F. Hadoke, Tiina Kipari, Jonathan R. Seckl & Karen E. Chapman. (2013) Modulation of 11β-Hydroxysteroid Dehydrogenase as a Strategy to Reduce Vascular Inflammation. Current Atherosclerosis Reports 15:5.
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V. V. Lipson, M. G. Shirobokova & O. N. Petrova. (2013) 11β-Hydroxysteroid dehydrogenase type 1, a target for development of oral antidiabetic drugs (Review). Pharmaceutical Chemistry Journal 47:2, pages 80-86.
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Gerhard Klebe. 2013. Drug Design. Drug Design 641 696 .
James S. Scott, Joanne deSchoolmeester, Elaine Kilgour, Rachel M. Mayers, Martin J. Packer, David Hargreaves, Stefan Gerhardt, Derek J. Ogg, Amanda Rees, Nidhal Selmi, Andrew Stocker, John G. Swales & Paul R. O. Whittamore. (2012) Novel Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor with Reduced Acyl Glucuronide Liability: The Discovery of 4-[4-(2-Adamantylcarbamoyl)-5- tert -butyl-pyrazol-1-yl]benzoic Acid (AZD8329) . Journal of Medicinal Chemistry 55:22, pages 10136-10147.
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James S. Scott, Adrian L. Gill, Linda Godfrey, Sam D. Groombridge, Amanda Rees, John Revill, Paul Schofield, Pernilla Sörme, Andrew Stocker, John G. Swales & Paul R.O. Whittamore. (2012) Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors. Bioorganic & Medicinal Chemistry Letters 22:21, pages 6756-6761.
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Eric Valeur, Serge Christmann-Franck, Franck Lepifre, Denis Carniato, Daniel Cravo, Christine Charon, Sophie Bozec, Djordje Musil, Per Hillertz, Liliane Doare, Fabien Schmidlin, Marc Lecomte, Melanie Schultz & Didier Roche. (2012) Structure-based design of 7-azaindole-pyrrolidine amides as inhibitors of 11β-hydroxysteroid dehydrogenase type I. Bioorganic & Medicinal Chemistry Letters 22:18, pages 5909-5914.
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James S. ScottSuzanne S. BowkerJoanne deSchoolmeesterStefan GerhardtDavid HargreavesElaine KilgourAdele LloydRachel M. MayersWilliam McCoullNicholas J. NewcombeDerek OggMartin J. PackerAmanda ReesJohn RevillPaul SchofieldNidhal SelmiJohn G. SwalesPaul R. O. Whittamore. (2012) Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor: Discovery of 2-[(3 S )-1-[5-(Cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic Acid (AZD4017) . Journal of Medicinal Chemistry 55:12, pages 5951-5964.
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Liming Zhang, Junhua Chen, Mengmeng Ning, Qingan Zou, Ying Leng & Jianhua Shen. (2012) Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice. Bioorganic & Medicinal Chemistry Letters 22:8, pages 2748-2752.
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James S. Scott, Peter Barton, Stuart N. L. Bennett, Joanne deSchoolmeester, Linda Godfrey, Elaine Kilgour, Rachel M. Mayers, Martin J. Packer, Amanda Rees, Paul Schofield, Nidhal Selmi, John G. Swales & Paul R. O. Whittamore. (2012) Reduction of acyl glucuronidation in a series of acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors: the discovery of AZD6925. MedChemComm 3:10, pages 1264.
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Xiangdong Su, Nigel Vicker, Mark P. Thomas, Fabienne Pradaux-Caggiano, Heather Halem, Michael D. Culler & Barry V. L. Potter. (2011) Discovery of Adamantyl Heterocyclic Ketones as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors. ChemMedChem 6:8, pages 1439-1451.
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Mark P ThomasBarry VL Potter. (2011) Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery. Future Medicinal Chemistry 3:3, pages 367-390.
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Clarence Hale & David J. St. Jean. 2011. Metabolic Syndrome. Metabolic Syndrome 423 458 .
Xiangdong Su, Fabienne Pradaux-Caggiano, Mark P. Thomas, Michelle W. Y. Szeto, Heather A. Halem, Michael D. Culler, Nigel Vicker & Barry V. L. Potter. (2010) Discovery of Adamantyl Ethanone Derivatives as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors. ChemMedChem 5:7, pages 1026-1044.
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Mariana Torres-Piedra, Rolffy Ortiz-Andrade, Rafael Villalobos-Molina, Narender Singh, Jose L. Medina-Franco, Scott P. Webster, Margaret Binnie, Gabriel Navarrete-Vázquez & Samuel Estrada-Soto. (2010) A comparative study of flavonoid analogues on streptozotocin–nicotinamide induced diabetic rats: Quercetin as a potential antidiabetic agent acting via 11β-Hydroxysteroid dehydrogenase type 1 inhibition. European Journal of Medicinal Chemistry 45:6, pages 2606-2612.
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Scott P. Webster, Margaret Binnie, Kirsty M.M. McConnell, Karen Sooy, Peter Ward, Michael F. Greaney, Andy Vinter, T. David Pallin, Hazel J. Dyke, Matthew I.A. Gill, Ines Warner, Jonathan R. Seckl & Brian R. Walker. (2010) Modulation of 11β-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles. Bioorganic & Medicinal Chemistry Letters 20:11, pages 3265-3271.
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Santhosh F. Neelamkavil, Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Lili Zhang & Giuseppe Terracina. (2009) The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors. Bioorganic & Medicinal Chemistry Letters 19:16, pages 4563-4565.
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Michael Siu, Theodore O. Johnson, Yong Wang, Sajiv K. Nair, Wendy D. Taylor, Stephan J. Cripps, Jean J. Matthews, Martin P. Edwards, Thomas A. Pauly, Jacques Ermolieff, Arturo Castro, Natilie A. Hosea, Amy LaPaglia, Andrea N. Fanjul & Jennifer E. Vogel. (2009) N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorganic & Medicinal Chemistry Letters 19:13, pages 3493-3497.
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Franck Lepifre, Serge Christmann-Franck, Didier Roche, Caroline Leriche, Denis Carniato, Christine Charon, Sophie Bozec, Liliane Doare, Fabien Schmidlin, Marc Lecomte & Eric Valeur. (2009) Discovery and structure-guided drug design of inhibitors of 11β-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold. Bioorganic & Medicinal Chemistry Letters 19:13, pages 3682-3685.
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Patrick W.F. Hadoke, Javaid Iqbal & Brian R. Walker. (2009) Therapeutic manipulation of glucocorticoid metabolism in cardiovascular disease. British Journal of Pharmacology 156:5, pages 689-712.
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Gerhard Klebe. 2009. Wirkstoffdesign. Wirkstoffdesign 459 498 .
R. R Ortiz‐Andrade, J. C. Sánchez‐Salgado, G. Navarrete‐Vázquez, S. P. Webster, M. Binnie, S. García‐Jiménez, I. León‐Rivera, P. Cigarroa‐Vázquez, R. Villalobos‐Molina & S. Estrada‐Soto. (2008) Antidiabetic and toxicological evaluations of naringenin in normoglycaemic and NIDDM rat models and its implications on extra‐pancreatic glucose regulation. Diabetes, Obesity and Metabolism 10:11, pages 1097-1104.
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Hermenegilda Moreno-Díaz, Rafael Villalobos-Molina, Rolffy Ortiz-Andrade, Daniel Díaz-Coutiño, Jose Luis Medina-Franco, Scott P. Webster, Margaret Binnie, Samuel Estrada-Soto, Maximiliano Ibarra-Barajas, Ismael León-Rivera & Gabriel Navarrete-Vázquez. (2008) Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides. Bioorganic & Medicinal Chemistry Letters 18:9, pages 2871-2877.
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