Literature DB >> 11472221

(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.

B B Lohray1, V B Lohray, A C Bajji, S Kalchar, R R Poondra, S Padakanti, R Chakrabarti, R K Vikramadithyan, P Misra, S Juluri, N V Mamidi, R Rajagopalan.   

Abstract

(-)DRF 2725 (6) is a phenoxazine analogue of phenyl propanoic acid. Compound 6 showed interesting dual activation of PPAR alpha and PPAR gamma. In insulin resistant db/db mice, 6 showed better reduction of plasma glucose and triglyceride levels as compared to rosiglitazone. Compound 6 has also shown good oral bioavailability and impressive pharmacokinetic characteristics. Our study indicates that 6 has great potential as a drug for diabetes and dyslipidemia.

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Year:  2001        PMID: 11472221     DOI: 10.1021/jm010143b

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


  13 in total

1.  Peroxisome proliferator-activated receptors target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis.

Authors:  Bernard Pirard
Journal:  J Comput Aided Mol Des       Date:  2003-11       Impact factor: 3.686

2.  The dual PPARalpha/gamma agonist, ragaglitazar, improves insulin sensitivity and metabolic profile equally with pioglitazone in diabetic and dietary obese ZDF rats.

Authors:  Lucy C Pickavance; Christian L Brand; Karsten Wassermann; John P H Wilding
Journal:  Br J Pharmacol       Date:  2005-02       Impact factor: 8.739

3.  Urinary phthalates and increased insulin resistance in adolescents.

Authors:  Leonardo Trasande; Adam J Spanier; Sheela Sathyanarayana; Teresa M Attina; Jan Blustein
Journal:  Pediatrics       Date:  2013-08-19       Impact factor: 7.124

Review 4.  PPARgamma as a new therapeutic target in inflammatory bowel diseases.

Authors:  L Dubuquoy; C Rousseaux; X Thuru; L Peyrin-Biroulet; O Romano; P Chavatte; M Chamaillard; P Desreumaux
Journal:  Gut       Date:  2006-09       Impact factor: 23.059

5.  Dandamycin and chandrananimycin E, benzoxazines from Streptomyces griseus.

Authors:  Emma C Barnes; Patricia Bezerra-Gomes; Markus Nett; Christian Hertweck
Journal:  J Antibiot (Tokyo)       Date:  2015-02-18       Impact factor: 2.649

6.  Ragaglitazar: a novel PPAR alpha PPAR gamma agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models.

Authors:  Ranjan Chakrabarti; Reeba K Vikramadithyan; Parimal Misra; Jagadheshan Hiriyan; Suryaprakash Raichur; Ravi K Damarla; Cynthia Gershome; Juluri Suresh; Ramanujam Rajagopalan
Journal:  Br J Pharmacol       Date:  2003-09-01       Impact factor: 8.739

7.  Preclinical pharmacokinetics and interspecies scaling of ragaglitazar, a novel biliary excreted PPAR dual activator.

Authors:  Venkata V Pavankuamr; C A Vinu; Ramesh Mullangi; Nuggehally R Srinivas
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2007 Jan-Mar       Impact factor: 2.441

Review 8.  [Future targets in the treatment of type 2 diabetes].

Authors:  Harald Stingl; Michael Roden
Journal:  Wien Klin Wochenschr       Date:  2004-04-30       Impact factor: 1.704

9.  Rat Urinary Bladder Carcinogenesis by Dual-Acting PPARalpha + gamma Agonists.

Authors:  Martin B Oleksiewicz; Jennifer Southgate; Lars Iversen; Frederikke L Egerod
Journal:  PPAR Res       Date:  2009-01-28       Impact factor: 4.964

10.  PPAR Agonists and Cardiovascular Disease in Diabetes.

Authors:  Anna C Calkin; Merlin C Thomas
Journal:  PPAR Res       Date:  2008       Impact factor: 4.964

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