A series of gemfibrozil analogues with a thiourea moiety embedded in the side chain was prepared and evaluated as HDL-elevating agents. Derivatives 8b, 9b, 9c, and 9d were found to be approximately as effective as gemfibrozil (1) for HDL cholesterol elevation.
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http://dx.doi.org/10.1016/s0960-894x(02)00435-3 | DOI Listing |
Clin Pharmacol Ther
June 2024
Pharmacokinetics, Dynamics, and Metabolism, Pfizer R&D, Pfizer Inc., Groton, Connecticut, USA.
J Ocul Pharmacol Ther
December 2020
Wellcome-Wolfson Institute for Experimental Medicine, School of Medicine, Dentistry and Biomedical Sciences, Queen's University Belfast, Northern Ireland, United Kingdom.
There is a lack of treatment for early diabetic retinopathy (DR), including blood-retina barrier (BRB) breakdown. The robust clinical benefit of fenofibrate in DR provides an opportunity to explore disease mechanisms and therapeutic targets. We have previously found that modified lipoproteins contribute to DR and that fenofibrate protects the inner BRB.
View Article and Find Full Text PDFEur J Med Chem
July 2020
Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi, 214122, PR China. Electronic address:
Novel methods for peptides structural modification and bioactivity optimization are highly needed in peptide-based drug discovery. Herein, we explored the use gemfibrozil (GFZ) as an albumin binder to enhance the stability and improve the bioactivity of peptides. Short-acting Xenopus glucagon-like peptide-1 (xGLP-1) analogues with anti-diabetic activity were selected as the starting point.
View Article and Find Full Text PDFMol Pharm
March 2020
Institute of Physics, University of Silesia, 75 Pulku Piechoty 1a, 41-500 Chorzow, Poland.
In this paper, broadband dielectric spectroscopy (BDS) has been applied to study the molecular dynamics and crystallization kinetics of the antihyperlipidemic active pharmaceutical ingredient (API), gemfibrozil (GEM), as well as its deuterated (dGEM) and methylated (metGEM) derivatives, characterized by different types and strengths of intermolecular interactions. Moreover, calorimetric and infrared measurements have been carried out to characterize the thermal properties of examined samples and to probe a change in the H-bonding pattern in GEM, respectively. We found that the dielectric spectra of all examined compounds, collected below the glass transition temperature (), reveal the presence of two secondary relaxations (β, γ).
View Article and Find Full Text PDFJ Clin Psychopharmacol
April 2020
Eastern State Hospital Lexington, KY. The Zucker Hillside Hospital Psychiatry Research, Northwell Health Glen Oaks Hofstra Northwell School of Medicine Hempstead and The Feinstein Institute for Medical Research Manhasset, New York University of Kentucky Mental Health Research Center Eastern State Hospital Lexington, KY
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