A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.
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http://dx.doi.org/10.1016/j.bmcl.2007.05.066 | DOI Listing |
Pharmaceutics
December 2024
Vinča Institute of Nuclear Sciences, National Institute of the Republic of Serbia, University of Belgrade, Mike Petrovića Alasa 12-14, 11001 Belgrade, Serbia.
Pathogen bacteria appear and survive on various surfaces made of steel or glass. The existence of these bacteria in different forms causes significant problems in healthcare facilities and society. Therefore, the surface engineering of highly potent antimicrobial coatings is highly important in the 21st century, a period that began with a series of epidemics.
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December 2024
COSYS/IMSE, Université Gustave Eiffel, Champs-sur-Marne, 77454 Marne-la-Vallée, Cedex 2, France.
RNA polymerase (NS5B), serves as a crucial target for pharmaceutical interventions aimed at combating the hepatitis C virus (HCV), which poses significant health challenges worldwide. The present research endeavors to explore and implement a variety of advanced molecular modeling techniques that aim to create and identify innovative and highly effective inhibitors that specifically target the RNA polymerase enzyme. In this study, a QSAR investigation was carried out on a set of thirty-eight isothiazole derivatives targeting NS5B inhibition and thus hepatitis C virus (HCV) treatment.
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November 2024
Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.
Small-molecule probes are powerful tools for studying biological systems and can serve as lead compounds for developing new therapeutics. Especially, nitrogen heterocycles are of considerable importance in the pharmaceutical field. These compounds are found in numerous bioactive structures.
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December 2024
Institute of Organic Chemistry and Macromolecular Chemistry, Faculty of Mathematics and Natural Sciences, Heinrich Heine University Düsseldorf, Universitätsstraße 1, D-40225 Düsseldorf, Germany.
(3-(pyrimidin-4-yl)-7-azaindoles) are synthetic hybrids of the naturally occurring alkaloids and and display a strong cytotoxic potential. We have recently shown that the novel derivative is highly cytotoxic in several lymphoma and leukemia cell lines as well as in primary patient-derived lymphoma and leukemia cells and predominantly targets cyclin-dependent kinases (CDKs). Here, we efficiently synthesized nine novel 2-aminopyridyl congeners (-), i.
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December 2024
Key Laboratory of Biopesticide and Chemical Biology, Ministry of Education, Fujian Agriculture and Forestry University, Fuzhou 350002, China.
Emamectin benzoate (EB) is a highly effective broad-spectrum insecticide and acaricide. However, because EB is easily degraded, the conventional formulations of EB are often overapplied. In this study, polylactic acid (PLA)-based microspheres were prepared using the modified solvent evaporation method for the controlled release of EB.
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