Literature DB >> 9599241

Isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds as hypoglycemic agents.

H Shinkai1, S Onogi, M Tanaka, T Shibata, M Iwao, K Wakitani, I Uchida.   

Abstract

Isoxazolidine-3,5-dione 2 (JTT-501), one of the cyclic malonic acid derivatives, was found to decrease blood glucose at an oral dose of 38 mg/kg/day in KKAy mice and is currently undergoing evaluation in phase II clinical trials. Further studies on a series of malonic acids and related compounds showed that the 1,3-dicarbonyl structure was important for insulin-sensitizing activity. Dimethyl malonate 10, which was selected as a successor for 2, was the optimum compound in a series of 1,3-dicarbonyl compounds and was more potent than the corresponding thiazolidine-2,4-dione 1.

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Year:  1998        PMID: 9599241     DOI: 10.1021/jm970771m

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  6 in total

1.  Differences in hepatotoxicity and gene expression profiles by anti-diabetic PPAR gamma agonists on rat primary hepatocytes and human HepG2 cells.

Authors:  Lei Guo; Lu Zhang; Yongming Sun; Levan Muskhelishvili; Ernice Blann; Stacey Dial; Leming Shi; Gary Schroth; Yvonne P Dragan
Journal:  Mol Divers       Date:  2006-09-21       Impact factor: 2.943

Review 2.  PPARgamma and its ligands: therapeutic implications in cardiovascular disease.

Authors:  Luis Villacorta; Francisco J Schopfer; Jifeng Zhang; Bruce A Freeman; Y Eugene Chen
Journal:  Clin Sci (Lond)       Date:  2009-02       Impact factor: 6.124

3.  3D QSAR studies on peroxisome proliferator-activated receptor gamma agonists using CoMFA and CoMSIA.

Authors:  Chenzhong Liao; Aihua Xie; Jiaju Zhou; Leming Shi; Zhibin Li; Xian-Ping Lu
Journal:  J Mol Model       Date:  2004-03-12       Impact factor: 1.810

Review 4.  Recent pharmacological developments on rhodanines and 2,4-thiazolidinediones.

Authors:  Ravinder Singh Bhatti; Sakshi Shah; Pawan Krishan; Jagir S Sandhu
Journal:  Int J Med Chem       Date:  2013-05-02

5.  A possible potential COVID-19 drug candidate: Diethyl 2-(2-(2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)acetyl)hydrazono)malonate: Docking of disordered independent molecules of a novel crystal structure, HSA/DFT/XRD and cytotoxicity.

Authors:  Mohcine Missioui; Musa A Said; Güneş Demirtaş; Joel T Mague; Ahlam Al-Sulami; Nadia S Al-Kaff; Youssef Ramli
Journal:  Arab J Chem       Date:  2021-11-28       Impact factor: 5.165

6.  Synthesis of 3,5-isoxazolidinediones and 1H-2,3-benzoxazine-1,4(3H)-diones from aliphatic oximes and dicarboxylic acid chlorides.

Authors:  Robert A Izydore; Joseph T Jones; Benjamin Mogesa; Ira N Swain; Ronda G Davis-Ward; Dwayne L Daniels; Felicia Frazier Kpakima; Sharnelle T Spaulding-Phifer
Journal:  J Org Chem       Date:  2014-03-21       Impact factor: 4.354

  6 in total

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