Suppr超能文献

双芳基三唑类化合物作为11β-羟基类固醇脱氢酶1型的选择性抑制剂

Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

作者信息

Aster Susan D, Graham Donald W, Kharbanda Divya, Patel Gool, Ponpipom Mitree, Santorelli Gina M, Szymonifka Michael J, Mundt Steven S, Shah Kashmira, Springer Marty S, Thieringer Rolf, Hermanowski-Vosatka Anne, Wright Samuel D, Xiao Jianying, Zokian Hratch, Balkovec James M

机构信息

Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.

出版信息

Bioorg Med Chem Lett. 2008 May 1;18(9):2799-804. doi: 10.1016/j.bmcl.2008.04.010. Epub 2008 Apr 9.

DOI:10.1016/j.bmcl.2008.04.010
PMID:18434143
Abstract

3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.

摘要

3-芳基-5-苯基-(1,2,4)-三唑被鉴定为11β-羟基类固醇脱氢酶1型（11β-HSD1）的选择性抑制剂。它们在体外和体内小鼠药效学（PD）模型中均具有活性。本文介绍了其合成方法及构效关系。

相似文献

1
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Bioorg Med Chem Lett. 2008 May 1;18(9):2799-804. doi: 10.1016/j.bmcl.2008.04.010. Epub 2008 Apr 9.
2
Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4359-62. doi: 10.1016/j.bmcl.2005.06.040.
3
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3405-11. doi: 10.1016/j.bmcl.2008.04.013. Epub 2008 Apr 10.
4
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3412-6. doi: 10.1016/j.bmcl.2008.04.014. Epub 2008 Apr 10.
5
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.
Bioorg Med Chem Lett. 2005 Dec 1;15(23):5266-9. doi: 10.1016/j.bmcl.2005.08.052. Epub 2005 Sep 26.
6
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
J Med Chem. 2008 May 22;51(10):2933-43. doi: 10.1021/jm701551j. Epub 2008 Apr 18.
7
Substituted phenyl triazoles as selective inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1.
Bioorg Med Chem Lett. 2011 Apr 1;21(7):2141-5. doi: 10.1016/j.bmcl.2011.01.125. Epub 2011 Feb 2.
8
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
J Med Chem. 2008 Jul 24;51(14):4068-71. doi: 10.1021/jm8004948. Epub 2008 Jun 26.
9
Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1551-4. doi: 10.1016/j.bmcl.2010.01.082. Epub 2010 Jan 25.
10
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1340-5. doi: 10.1016/j.bmcl.2008.01.020. Epub 2008 Jan 11.

引用本文的文献

1
Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
ChemMedChem. 2011 Aug 1;6(8):1439-51. doi: 10.1002/cmdc.201100144. Epub 2011 May 23.
2
11β-hydroxysteroid dehydrogenases and the brain: from zero to hero, a decade of progress.
Front Neuroendocrinol. 2011 Aug;32(3):265-86. doi: 10.1016/j.yfrne.2010.12.001. Epub 2010 Dec 7.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型，支持多种主流文档格式。

立即体验