Literature DB >> 17451949

Discovery and SAR development of thienopyridones: a class of small molecule AMPK activators.

Gang Zhao1, Rajesh R Iyengar, Andrew S Judd, Barbara Cool, William Chiou, Lemma Kifle, Ernst Frevert, Hing Sham, Philip R Kym.   

Abstract

AMP-activated protein kinase (AMPK) is well established as a sensor and regulator of intracellular and whole-body energy metabolism. A high-throughput screen was performed in order to identify chemotypes that are bound by AMPK. A novel thienopyridone compound (1) was identified and subsequently optimized. The structure-activity relationships that emerged from this effort are described.

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Year:  2007        PMID: 17451949     DOI: 10.1016/j.bmcl.2007.04.011

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


  6 in total

1.  Development of novel adenosine monophosphate-activated protein kinase activators.

Authors:  Jih-Hwa Guh; Wei-Ling Chang; Jian Yang; Su-Lin Lee; Shuo Wei; Dasheng Wang; Samuel K Kulp; Ching-Shih Chen
Journal:  J Med Chem       Date:  2010-03-25       Impact factor: 7.446

2.  Turning enzymes ON with small molecules.

Authors:  Julie A Zorn; James A Wells
Journal:  Nat Chem Biol       Date:  2010-03       Impact factor: 15.040

Review 3.  The Gewald multicomponent reaction.

Authors:  Yijun Huang; Alexander Dömling
Journal:  Mol Divers       Date:  2010-02-27       Impact factor: 2.943

4.  A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis.

Authors:  Jorge E Gómez-Galeno; Qun Dang; Thanh H Nguyen; Serge H Boyer; Matthew P Grote; Zhili Sun; Mingwei Chen; William A Craigo; Paul D van Poelje; Deidre A MacKenna; Edward E Cable; Paul A Rolzin; Patricia D Finn; Bert Chi; David L Linemeyer; Scott J Hecker; Mark D Erion
Journal:  ACS Med Chem Lett       Date:  2010-08-30       Impact factor: 4.345

5.  AMPK regulates metabolic actions of glucocorticoids by phosphorylating the glucocorticoid receptor through p38 MAPK.

Authors:  Nancy Nader; Sinnie Sin Man Ng; George I Lambrou; Panagiota Pervanidou; Yonghong Wang; George P Chrousos; Tomoshige Kino
Journal:  Mol Endocrinol       Date:  2010-07-21

6.  Advanced palladium free approach to the synthesis of substituted alkene oxindoles via aluminum-promoted Knoevenagel reaction.

Authors:  Daria S Novikova; Tatyana A Grigoreva; Andrey A Zolotarev; Alexander V Garabadzhiu; Vyacheslav G Tribulovich
Journal:  RSC Adv       Date:  2018-10-10       Impact factor: 3.361

  6 in total

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