Literature DB >> 19427223

Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy.

Tomoharu Iino1, Noriaki Hashimoto, Kaori Sasaki, Sumika Ohyama, Riki Yoshimoto, Hideka Hosaka, Takuro Hasegawa, Masato Chiba, Yasufumi Nagata, Jun-ichi Eiki, Teruyuki Nishimura.   

Abstract

The optimization of our lead GK activator 2a to 3-[(1S)-2-hydroxy-1-methylethoxy]-5-[4-(methylsulfonyl)phenoxy]-N-1,3-thiazol-2-ylbenzamide (6g), a potent GK activator with good oral availability, is described, including to uncouple the relationship between potency and hydrophobicity. Following oral administration, this compound exhibited robust glucose lowering in diabetic model rodents.

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Year:  2009        PMID： 19427223     DOI： 10.1016/j.bmc.2009.04.040

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  9 in total

1.  Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM.

Authors:  Kaapjoo Park; Byoung Moon Lee; Kwan Hoon Hyun; Taedong Han; Dong Hoon Lee; Hyun Ho Choi
Journal:  ACS Med Chem Lett       Date:  2015-01-14       Impact factor: 4.345

2.  Control of beta cell function and proliferation in mice stimulated by small-molecule glucokinase activator under various conditions.

Authors:  A Nakamura; Y Togashi; K Orime; K Sato; J Shirakawa; M Ohsugi; N Kubota; T Kadowaki; Y Terauchi
Journal:  Diabetologia       Date:  2012-03-29       Impact factor: 10.122

3.  Chronic treatment with a glucokinase activator delays the onset of hyperglycaemia and preserves beta cell mass in the Zucker diabetic fatty rat.

Authors:  M Futamura; J Yao; X Li; R Bergeron; J-L Tran; E Zycband; J Woods; Y Zhu; Q Shao; H Maruki-Uchida; H Goto-Shimazaki; R B Langdon; M D Erion; J Eiki; Y-P Zhou
Journal:  Diabetologia       Date:  2012-01-11       Impact factor: 10.122

4.  Glucokinase activation ameliorates ER stress-induced apoptosis in pancreatic β-cells.

Authors:  Jun Shirakawa; Yu Togashi; Eri Sakamoto; Mitsuyo Kaji; Kazuki Tajima; Kazuki Orime; Hideaki Inoue; Naoto Kubota; Takashi Kadowaki; Yasuo Terauchi
Journal:  Diabetes       Date:  2013-06-25       Impact factor: 9.461

5.  Effect of long-term treatment with a small-molecule glucokinase activator on glucose metabolism, lipid profiles and hepatic function.

Authors:  Akinobu Nakamura; Hiroko Shimazaki; Sumika Ohyama; Junichi Eiki; Yasuo Terauchi
Journal:  J Diabetes Investig       Date:  2011-08-02       Impact factor: 4.232

6.  Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents.

Authors:  Sraa Abu-Melha; Mastoura M Edrees; Heba H Salem; Nabila A Kheder; Sobhi M Gomha; Mohamad R Abdelaziz
Journal:  Molecules       Date:  2019-02-01       Impact factor: 4.411

7.  Dynamic localization of glucokinase and its regulatory protein in hypothalamic tanycytes.

Authors:  Magdiel Salgado; Estefanía Tarifeño-Saldivia; Patricio Ordenes; Carola Millán; María José Yañez; Paula Llanos; Marcos Villagra; Roberto Elizondo-Vega; Fernando Martínez; Francisco Nualart; Elena Uribe; María de Los Angeles García-Robles
Journal:  PLoS One       Date:  2014-04-16       Impact factor: 3.240

8.  Stereoselective synthesis, X-ray analysis, computational studies and biological evaluation of new thiazole derivatives as potential anticancer agents.

Authors:  Yahia N Mabkhot; Mohammed M Alharbi; Salim S Al-Showiman; Hazem A Ghabbour; Nabila A Kheder; Saied M Soliman; Wolfgang Frey
Journal:  Chem Cent J       Date:  2018-05-11       Impact factor: 4.215

9.  Eco-Friendly Synthesis, Characterization and Biological Evaluation of Some Novel Pyrazolines Containing Thiazole Moiety as Potential Anticancer and Antimicrobial Agents.

Authors:  Mastoura M Edrees; Sraa Abu- Melha; Amirah M Saad; Nabila A Kheder; Sobhi M Gomha; Zeinab A Muhammad
Journal:  Molecules       Date:  2018-11-14       Impact factor: 4.411
  9 in total

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