Literature DB >> 18440811

4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Yuping Zhu1, Steven H Olson, Anne Hermanowski-Vosatka, Steven Mundt, Kashmira Shah, Marty Springer, Rolf Thieringer, Samuel Wright, Jianying Xiao, Hratch Zokian, James M Balkovec.   

Abstract

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

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Year:  2008        PMID: 18440811     DOI: 10.1016/j.bmcl.2008.04.013

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Human hydroxysteroid dehydrogenases and pre-receptor regulation: insights into inhibitor design and evaluation.

Authors:  Trevor M Penning
Journal:  J Steroid Biochem Mol Biol       Date:  2011-01-25       Impact factor: 4.292

2.  Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.

Authors:  Pengcheng P Shao; Feng Ye; Prasun K Chakravarty; James B Herrington; Ge Dai; Randal M Bugianesi; Rodolfo J Haedo; Andrew M Swensen; Vivien A Warren; McHardy M Smith; Maria L Garcia; Owen B McManus; Kathryn A Lyons; Xiaohua Li; Mitchell Green; Nina Jochnowitz; Erin McGowan; Shruti Mistry; Shu-Yu Sun; Catherine Abbadie; Gregory J Kaczorowski; Joseph L Duffy
Journal:  ACS Med Chem Lett       Date:  2013-09-08       Impact factor: 4.345

Review 3.  A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.

Authors:  Tao Liu; James P Beck; Junliang Hao
Journal:  RSC Med Chem       Date:  2022-01-19

Review 4.  11β-hydroxysteroid dehydrogenases and the brain: from zero to hero, a decade of progress.

Authors:  Caitlin S Wyrwoll; Megan C Holmes; Jonathan R Seckl
Journal:  Front Neuroendocrinol       Date:  2010-12-07       Impact factor: 8.606

5.  Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Nigel Vicker; Mark P Thomas; Fabienne Pradaux-Caggiano; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-05-23       Impact factor: 3.466

  5 in total

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