Heterocyclic compounds hold a huge and recognized place in the field of medicinal chemistry thanks to their multiple biological activities. Their synthetic pathways allow their easy and rapid access due to different bond-forming methodologies and provide a huge amount of multi-functionalized compounds for drug delivery. The syntheses of heterocyclic compounds are today well known for the majority, described and reviewed in an extensive literature. In this review, we choose to gather and classify available information concerning the biological activities of quinoxaline-based compounds annulated at bond a containing one and more nitrogen atoms in the fused azole ring.
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http://dx.doi.org/10.2174/0929867327666200206114936 | DOI Listing |
J Diet Suppl
January 2025
Department of Biomedical and Biotechnological Sciences, University of Catania, Catania, Italy.
Background: Several epidemiological studies and intervention trials have demonstrated that grapes and blueberries, which are rich in flavanols, can lower the risk of cardiovascular disease. However, the mechanisms of action of these compounds remain unclear due to their low bioavailability.
Objective: This study aimed to characterize the sensory properties, blood flow velocity, and oxidative stress of a polyphenol rich grape and blueberry extract (PEGB) containing approximately 16% flavanols (11% monomers and 4% dimers).
EJNMMI Radiopharm Chem
January 2025
Division of Nuclear Medicine, Department of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, Vienna, Austria.
Background: Poly (ADP-ribose) polymerase (PARP) enzymes are crucial for the repair of DNA single-strand breaks and have become key therapeutic targets in homologous recombination-deficient cancers, including prostate cancer. To enable non-invasive monitoring of PARP-1 expression, several PARP-1-targeting positron emission tomography (PET) tracers have been developed. Here, we aimed to preclinically investigate [carbonyl-C]DPQ as an alternative PARP-1 PET tracer as it features a strongly distinct chemotype compared to the frontrunners [F]FluorThanatrace and [F]PARPi.
View Article and Find Full Text PDFOrg Lett
January 2025
Department of Chemistry, School of Science, China Pharmaceutical University, Nanjing 211198, People's Republic of China.
The development and enantioselective synthesis of two types of -symmetric spirobi[dihydrophenalene] structures is reported. The reaction proceeds via rhodium-catalyzed 2-fold asymmetric conjugate arylation of dienones followed by BF·OEt-promoted spirocyclization to give the enantiopure spiro products. Additive-dependent chemodivergent synthesis of 3,3'-diarylated 2,2',3,3'-tetrahydro-1,1'-spirobi[phenalene]-9,9'-diols (3,3'-Ar-SPHENOLs) and the corresponding spiro diary ethers from the same intermediate is achieved.
View Article and Find Full Text PDFLangmuir
January 2025
Unilever R&D, 40 Merrit Boulevard, Trumbull, Connecticut 06611, United States.
Mixtures of multiple surfactants that have superior performance to the individual components are highly sought-after commercially. Mixtures with a reduced Krafft point () are particularly useful as they enable applications at lower temperatures. Such an example is the soap maker's eutectic: the mixture of sodium laurate (NaL) and sodium oleate (NaOl).
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow-226031, India.
Herein, we report a photocatalytic method for oxidative hydroacylation with alcohols. Under photoirradiation and a catalytic amount of TBADT, different electrophiles (azodicarboxylates, -phenylmaleimide, benzylidenemalononitrile and phenyl vinyl sulfone) underwent hydroacylation with alcohols in good yields. The method was also applied to achieve a convenient synthesis of the anti-depressant drug moclobemide.
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