Literature DB >> 16446092

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.

Chunqiu Lai1, Rebecca J Gum, Melissa Daly, Elizabeth H Fry, Charles Hutchins, Celerino Abad-Zapatero, Thomas W von Geldern.   

Abstract

A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53, with an IC(50) of 0.57microM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.

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Year:  2006        PMID： 16446092     DOI： 10.1016/j.bmcl.2006.01.014

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


  12 in total

1.  Microwave-assisted sequential one-pot protocol to benzothiadiazin-3-one-1,1-dioxides via a copper-catalyzed N-arylation strategy.

Authors:  Alan Rolfe; Paul R Hanson
Journal:  Tetrahedron Lett       Date:  2009-12-16       Impact factor: 2.415

2.  Cobalt Regulates Activation of Camk2α in Neurons by Influencing Fructose 1,6-bisphosphatase 2 Quaternary Structure and Subcellular Localization.

Authors:  Przemysław Duda; Bartosz Budziak; Dariusz Rakus
Journal:  Int J Mol Sci       Date:  2021-04-30       Impact factor: 5.923

3.  In silico identification of structure requirement for novel thiazole and oxazole derivatives as potent fructose 1,6-bisphosphatase inhibitors.

Authors:  Ming Hao; Xiaole Zhang; Hong Ren; Yan Li; Shuwei Zhang; Fang Luo; Mingjuan Ji; Guohui Li; Ling Yang
Journal:  Int J Mol Sci       Date:  2011-11-18       Impact factor: 5.923

4.  The role of liver fructose-1,6-bisphosphatase in regulating appetite and adiposity.

Authors:  Sherley Visinoni; Nurul Fathiah Izzati Khalid; Christos N Joannides; Arthur Shulkes; Mildred Yim; Jon Whitehead; Tony Tiganis; Benjamin J Lamont; Jenny M Favaloro; Joseph Proietto; Sofianos Andrikopoulos; Barbara C Fam
Journal:  Diabetes       Date:  2012-05       Impact factor: 9.461

5.  Quadruple space-group ambiguity owing to rotational and translational noncrystallographic symmetry in human liver fructose-1,6-bisphosphatase.

Authors:  Armin Ruf; Tim Tetaz; Brigitte Schott; Catherine Joseph; Markus G Rudolph
Journal:  Acta Crystallogr D Struct Biol       Date:  2016-10-28       Impact factor: 7.652

6.  The liver: Key in regulating appetite and body weight.

Authors:  Barbara C Fam; Christos N Joannides; Sofianos Andrikopoulos
Journal:  Adipocyte       Date:  2012-10-01       Impact factor: 4.534

7.  Synthesis and screening of antibacterial and antifungal activity of 5-chloro-1,3-benzoxazol-2(3 h)-one derivatives.

Authors:  Priya R Modiya; Chhaganbhai N Patel
Journal:  Org Med Chem Lett       Date:  2012-08-01

8.  Toward the prediction of FBPase inhibitory activity using chemoinformatic methods.

Authors:  Ming Hao; Shuwei Zhang; Jieshan Qiu
Journal:  Int J Mol Sci       Date:  2012-06-07       Impact factor: 6.208

9.  Structures of Leishmania Fructose-1,6-Bisphosphatase Reveal Species-Specific Differences in the Mechanism of Allosteric Inhibition.

Authors:  Meng Yuan; Montserrat G Vásquez-Valdivieso; Iain W McNae; Paul A M Michels; Linda A Fothergill-Gilmore; Malcolm D Walkinshaw
Journal:  J Mol Biol       Date:  2017-09-04       Impact factor: 5.469

10.  Polymyxins and quinazolines are LSD1/KDM1A inhibitors with unusual structural features.

Authors:  Valentina Speranzini; Dante Rotili; Giuseppe Ciossani; Simona Pilotto; Biagina Marrocco; Mariantonietta Forgione; Alessia Lucidi; Federico Forneris; Parinaz Mehdipour; Sameer Velankar; Antonello Mai; Andrea Mattevi
Journal:  Sci Adv       Date:  2016-09-09       Impact factor: 14.136
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