Literature DB >> 32206235

Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study.

Pasquale Linciano1, Barbara De Filippis2, Alessandra Ammazzalorso2, Pasquale Amoia2, Felisa Cilurzo2, Marialuigia Fantacuzzi2, Letizia Giampietro2, Cristina Maccallini2, Charlotte Petit3, Rosa Amoroso2.   

Abstract

PPAR agonists represent a new therapeutic opportunity for the prevention and treatment of neurodegenerative disorders, but their pharmacological success depends on favourable pharmacokinetic properties and capability to cross the BBB. In this study, we assayed some PPAR agonists previously synthesized by us for their physicochemical properties, with particular references to lipophilicity, solubility and permeability profiles, using the PAMPA. Although tested compounds showed high lipophilicity and low aqueous solubility, the results revealed a good overall druggability profile, encouraging further studies in the field of neurodegenerative diseases. This journal is © The Royal Society of Chemistry 2019.

Entities:  

Year:  2019        PMID： 32206235      PMCID： PMC7069374          DOI： 10.1039/c9md00286c

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  41 in total

Review 1.  Methodologies to assess drug permeation through the blood-brain barrier for pharmaceutical research.

Authors:  Céline Passeleu-Le Bourdonnec; Pierre-Alain Carrupt; Jean Michel Scherrmann; Sophie Martel
Journal:  Pharm Res       Date:  2013-06-26       Impact factor: 4.200

2.  Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism.

Authors:  Barbara De Filippis; Antonella Giancristofaro; Alessandra Ammazzalorso; Alessandra D'Angelo; Marialuigia Fantacuzzi; Letizia Giampietro; Cristina Maccallini; Michele Petruzzelli; Rosa Amoroso
Journal:  Eur J Med Chem       Date:  2011-08-23       Impact factor: 6.514

Review 3.  The Positive Regulation of eNOS Signaling by PPAR Agonists in Cardiovascular Diseases.

Authors:  Cristina Maccallini; Adriano Mollica; Rosa Amoroso
Journal:  Am J Cardiovasc Drugs       Date:  2017-08       Impact factor: 3.571

Review 4.  Drug penetration across the blood-brain barrier: an overview.

Authors:  V Mangas-Sanjuan; M González-Alvarez; I Gonzalez-Alvarez; M Bermejo
Journal:  Ther Deliv       Date:  2010-10

5.  PPAR-γ agonist GL516 reduces oxidative stress and apoptosis occurrence in a rat astrocyte cell line.

Authors:  Letizia Giampietro; Marialucia Gallorini; Barbara De Filippis; Rosa Amoroso; Amelia Cataldi; Viviana di Giacomo
Journal:  Neurochem Int       Date:  2019-04-01       Impact factor: 3.921

6.  High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.

Authors:  F Wohnsland; B Faller
Journal:  J Med Chem       Date:  2001-03-15       Impact factor: 7.446

Review 7.  Role of PPAR receptor in different diseases and their ligands: Physiological importance and clinical implications.

Authors:  Agha Zeeshan Mirza; Ismail I Althagafi; Hina Shamshad
Journal:  Eur J Med Chem       Date:  2019-02-01       Impact factor: 6.514

Review 8.  Development of Fibrates as Important Scaffolds in Medicinal Chemistry.

Authors:  Letizia Giampietro; Alessandra Ammazzalorso; Rosa Amoroso; Barbara De Filippis
Journal:  ChemMedChem       Date:  2019-05-07       Impact factor: 3.466

Review 9.  Estimating drug solubility in the gastrointestinal tract.

Authors:  J B Dressman; M Vertzoni; K Goumas; C Reppas
Journal:  Adv Drug Deliv Rev       Date:  2007-05-29       Impact factor: 15.470

10.  Fibrate-derived N-(methylsulfonyl)amides with antagonistic properties on PPARα.

Authors:  Alessandra Ammazzalorso; Alessandra D'Angelo; Antonella Giancristofaro; Barbara De Filippis; Mauro Di Matteo; Marialuigia Fantacuzzi; Letizia Giampietro; Pasquale Linciano; Cristina Maccallini; Rosa Amoroso
Journal:  Eur J Med Chem       Date:  2012-10-23       Impact factor: 6.514
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  1 in total

1.  Synthesis and Biological Evaluation of Halogenated E-Stilbenols as Promising Antiaging Agents.

Authors:  Ester Sara Di Filippo; Letizia Giampietro; Barbara De Filippis; Marwa Balaha; Vincenzo Ferrone; Marcello Locatelli; Tiziana Pietrangelo; Angela Tartaglia; Rosa Amoroso; Stefania Fulle
Journal:  Molecules       Date:  2020-12-07       Impact factor: 4.411
  1 in total

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