Adamantyl carboxamides and acetamides as potent human 11β-hydroxysteroid dehydrogenase type 1 inhibitors
暂无分享,去创建一个
Xiangdong Su | Mark P. Thomas | Mark P Thomas | B. Potter | M. Culler | N. Vicker | H. Halem | Nigel Vicker | Barry V.L. Potter | Michael D. Culler | Heather A. Halem | Cecile Moutrille | Xiangdong Su | Cécile Moutrille
[1] R. Gregg,et al. Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1. , 2010, Bioorganic & medicinal chemistry letters.
[2] A. Odermatt,et al. A rapid screening assay for inhibitors of 11β-hydroxysteroid dehydrogenases (11β-HSD): flavanone selectively inhibits 11β-HSD1 reductase activity , 2003, Molecular and Cellular Endocrinology.
[3] B. Walker,et al. Printed in U.S.A. Copyright © 2001 by The Endocrine Society Minireview: 11�-Hydroxysteroid Dehydrogenase Type 1— A Tissue-Specific Amplifier of Glucocorticoid Action* , 2000 .
[4] B. Potter,et al. Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery. , 2011, Future medicinal chemistry.
[5] Mark P Thomas,et al. Adamantyl Ethanone Pyridyl Derivatives: Potent and Selective Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 , 2011, ChemMedChem.
[6] R. Ge,et al. 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors as Promising Therapeutic Drugs for Diabetes: Status and Development , 2010 .
[7] B. Potter,et al. Discovery of Adamantyl Ethanone Derivatives as Potent 11β‐Hydroxysteroid Dehydrogenase Type 1 (11β‐HSD1) Inhibitors , 2010, ChemMedChem.
[8] T. Kowalski,et al. 11β-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents , 2009, Expert opinion on therapeutic patents.
[9] Mark P Thomas,et al. Synthesis and evaluation of thiadiazole derivatives as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 , 2012 .
[10] Richard Barnett. Diabetes , 1904, The Lancet.
[11] J. Flier,et al. Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice. , 2003, The Journal of clinical investigation.
[12] J. Seckl,et al. Local Amplification of Glucocorticoids by 11β‐Hydroxysteroid Dehydrogenase Type 1 and Its Role in the Inflammatory Response , 2006, Annals of the New York Academy of Sciences.
[13] R. Thieringer,et al. 11β-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice , 2005, The Journal of experimental medicine.
[14] K. Svenson,et al. Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model. , 2009, Journal of medicinal chemistry.
[15] J. Flier,et al. Novel adipose tissue-mediated resistance to diet-induced visceral obesity in 11 beta-hydroxysteroid dehydrogenase type 1-deficient mice. , 2004, Diabetes.
[16] J. Rosenstock,et al. The 11-β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor INCB13739 Improves Hyperglycemia in Patients With Type 2 Diabetes Inadequately Controlled by Metformin Monotherapy , 2010, Diabetes Care.
[17] K. Longenecker,et al. Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors , 2007 .
[18] T. Mune,et al. NAD(+)-dependent isoform of 11 beta-hydroxysteroid dehydrogenase. Cloning and characterization of cDNA from sheep kidney. , 1994, The Journal of biological chemistry.
[19] E. Valeur,et al. Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I. , 2009, Bioorganic & medicinal chemistry letters.
[20] Edwards,et al. 11 b-Hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress , 1997 .
[21] Warszawski Uniwersytet Medyczny,et al. Diabetes care , 2019, Health at a Glance.
[22] H. Tutill,et al. Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design. , 2008, Bioorganic & medicinal chemistry.
[23] B. Potter,et al. Discovery of novel inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 , 2009, Molecular and Cellular Endocrinology.
[24] R. Thieringer,et al. Inhibition of 11β-HSD1 as a novel treatment for the metabolic syndrome: do glucocorticoids play a role? , 2005, Expert review of cardiovascular therapy.
[25] Minghan Wang,et al. Nutrition & Metabolism BioMed Central Review The role of glucocorticoid action in the pathophysiology of the Metabolic Syndrome , 2004 .
[26] C. Kim,et al. Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group. , 2011, Bioorganic & medicinal chemistry letters.
[27] Mark P Thomas,et al. Discovery of Adamantyl Heterocyclic Ketones as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors , 2011, ChemMedChem.
[28] Minghan Wang,et al. Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. , 2008, Journal of medicinal chemistry.
[29] Jiandong Zhang,et al. 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). , 2010, Journal of medicinal chemistry.
[30] B. Walker,et al. Pathophysiology of modulation of local glucocorticoid levels by 11β-hydroxysteroid dehydrogenases , 2001, Trends in Endocrinology & Metabolism.
[31] John J. Mullins,et al. Improved Lipid and Lipoprotein Profile, Hepatic Insulin Sensitivity, and Glucose Tolerance in 11β-Hydroxysteroid Dehydrogenase Type 1 Null Mice* , 2001, The Journal of Biological Chemistry.
[32] J. Flier,et al. Adipocyte-specific glucocorticoid inactivation protects against diet-induced obesity. , 2005, Diabetes.
[33] Jeremy W Tomlinson,et al. 11 (cid:1) -Hydroxysteroid Dehydrogenase Type 1: A Tissue-Specific Regulator of Glucocorticoid Response , 2004 .