Pre-clinical Pharmacokinetics and toxicologic evaluation of 5-(4-chloro-benzylidene)-3-(4-methyl-benzyl)-thiazolidine-2,4-dione(GQ-2).

• Grant number: 12/07049-2
• Support Opportunities: Scholarships in Brazil - Master
• Start date: November 01, 2012
• End date: July 31, 2013
• Field of knowledge: Biological Sciences - Pharmacology
• Principal Investigator: Rosangela Gonçalves Peccinini
• Grantee: Carla Monalizi Vieira
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Diabetes mellitus type 2 (DM2) is a metabolic disorder characterized by decreased activity and secretion of insulin. Increased longevity, combined with the growing prevalence of obesity, made this disease become the largest problem for the public health worldwide. Currently, only the drug pioglitazone of the class of thiazolidinediones is available in the market for the treatment of DM2, however this drug is under ANVISA's sight for its carcinogenic potential and cardiac toxicity. These compounds act by activating the nuclear receptor PPAR gamma which increases sensitivity to insulin in its targeted tissues. MOURÃO et al (2006) developed the compound 5 - (4-chloro-benzylidene) -3 - (4-methyl-benzyl)-thiazolidine-2 ,4-dione (GQ-2) with a potential hypoglycemic activity. The drug investigation of its molecular and metabolic effects in "swiss" obese mice showed a reduction in the standard insulin, glucose and leptin levels, associated with increased insulin sensitivity. Furthermore, the animals showed a reduction in body weight gain due to diminished fluids retention. This project aims to evaluate the pharmacokinetic profile and the toxicity in liver and kidney of the compound GQ-2 in Wistar rats.

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

VIEIRA, Carla Monalizi. Farmacocinética pré-clínica e avaliação toxicológica preliminar da nova tiazolidinadiona desenvolvida para o tratamento do diabetes mellitus tipo 2: 5-(4-cloro-benzilideno)-3-(4-metil-benzil)-tiazolidina-2,4-diona (GQ-2). 2013. Master's Dissertation - Universidade Estadual Paulista (Unesp). Faculdade de Ciências Farmacêuticas. Araraquara Araraquara.