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Discovery of thiazolidine-2,4-dione/biphenylcarbonitrile hybrid as dual PPAR α/γ modulator with antidiabetic effect: In vitro, in silico and in vivo approaches(†).
MedLine Citation:
PMID:  23289972     Owner:  NLM     Status:  Publisher    
A small series of thiazolidine-2,4-dione and barbituric acid derivatives 1-4 was prepared using a short synthetic route, and all compounds were characterized by elemental analysis, mass spectrometry and NMR ((1) H, (13) C) spectroscopy. Their in vitro relative expression of PPARα and PPARγ was evaluated. Compound 1 showed an increase in the mRNA expression of both PPAR isoforms, as well as the GLUT-4 levels. The antidiabetic activity of compound 1 was determined at 50 mg/Kg single dose using a non insulin dependent diabetes mellitus rat model (NIDDM). The results indicated a significant decrease of plasma glucose levels. Additionally, we performed a molecular docking of compound 1 into the ligand binding pocket of PPARα and PPARγ. In these binding models, compound 1 may bind into the active site of both isoforms showing important short contacts with the PPARγ residues: Tyr 473, His 449, Ser 289, His 323; and PPARα residues: Tyr 464, His 440, Ser 280 and Tyr 314 © 2013 John Wiley & Sons A/S.
Sergio Hidalgo-Figueroa; Juan José Ramírez-Espinosa; Samuel Estrada-Soto; Julio César Almanza-Pérez; Rubén Román-Ramos; Francisco Javier Alarcón-Aguilar; Jesús Vladimir Hernández-Rosado; Hermenegilda Moreno-Díaz; Daniel Díaz-Coutiño; Gabriel Navarrete-Vázquez
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-5
Journal Detail:
Title:  Chemical biology & drug design     Volume:  -     ISSN:  1747-0285     ISO Abbreviation:  Chem Biol Drug Des     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101262549     Medline TA:  Chem Biol Drug Des     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
© 2013 John Wiley & Sons A/S.
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, Chamilpa, Cuernavaca Mor, 62209, México.
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