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Biofilm inhibiting properties of compounds from the leaves of Warburgia ugandensis Sprague subsp ugandensis against Candida and staphylococcal biofilms. KU Leuven

Purity Kipanga, Maoxuan Liu, Sujogya K Panda, Anh Hung Mai, Cedrick Veryser, Luc Van Puyvelde, Wim De Borggraeve, Patrick Van Dijck, Josphat Matasyoh, Walter Luyten, et al.
ETHNOPHARMACOLOGICAL RELEVANCE: Warburgia ugandensis Sprague subspecies ugandensis is a plant widely distributed in Eastern, Central and Southern Africa. In humans, it is used to treat respiratory infections, tooth aches, malaria, skin infections, venereal diseases, diarrhea, fevers and aches. AIM OF THE STUDY: This study aims to identify the bioactive compounds against clinically important biofilm-forming strains of Candida and staphylococci ...

Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. KU Leuven

Ting Xiao, Jia-Fan Tang, Ge Meng, Christophe Pannecouque, Yuan-Yuan Zhu, Gen-Yan Liu, Zhi-Qiang Xu, Feng-Shou Wu, Shuang-Xi Gu, Fen-Er Chen, et al.
A series of indazolyl-substituted piperidin-4-yl-aminopyrimidines (IPAPYs) were designed from two potent HIV-1 NNRTIs piperidin-4-yl-aminopyrimidine 3c and diaryl ether 4 as the lead compounds by molecular hybridization strategy. The target molecules 5a-q were synthesized and evaluated for their anti-HIV activities and cytotoxicities in MT-4 cells. 5a-q displayed moderate to excellent activities against wild-type (WT) HIV-1 with EC50 values ...

Superior inhibition of influenza virus hemagglutinin-mediated fusion by indole-substituted spirothiazolidinones KU Leuven

Gokce Cihan-Ustundag, Muhammet Zopun, Evelien Vanderlinden, Elif Ozkirimli, Leentje Persoons, Gultaze Capan, Lieve Naesens
The influenza virus hemagglutinin (HA) mediates membrane fusion after viral entry by endocytosis. The fusion process requires drastic low pH-induced HA refolding and is prevented by arbidol and tert-butylhydroquinone (TBHQ). We here report a class of superior inhibitors with indole-substituted spirothiazolidinone structure. The most active analogue 5f has an EC50 value against influenza A/H3N2 virus of 1 nM and selectivity index of almost 2000. ...

Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors KU Leuven

Sheng Han, Yali Sang, Yan Wu, Yuan Tao, Christophe Pannecouque, Erik De Clercq, Chunlin Zhuang, Fen-Er Chen
The fragment hopping approach is widely applied in drug development. A series of diarylpyrimidines (DAPYs) were obtained by hopping the thioacetamide scaffold to novel human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase inhibitors (NNRTIs) to address the cytotoxicity issue of Etravirine and Rilpivirine. Although the new compounds (11a-l) in the first-round optimization possessed less potent anti-viral activity, they ...

Antitumor and antiviral activities of 4-substituted 1,2,3-triazolyl-2,3-dibenzyl-L-ascorbic acid derivatives KU Leuven

Andrijana Mescic Macan, Anja Harej, Ines Cazin, Marko Klobucar, Visnja Stepanic, Kresimir Pavelic, Sandra Kraljevic Pavelic, Dominique Schols, Robert Snoeck, Graciela Andrei, et al.
Two series of 6-(1,2,3-triazolyl)-2,3-dibenzyl-l-ascorbic acid derivatives with the hydroxyethylene (8a-8u) and ethylidene linkers (10c-10p) were synthesized and evaluated for their antiproliferative activity against seven malignant tumor cell lines and antiviral activity against a broad range of viruses. Conformationally unrestricted spacer between the lactone and 1,2,3-triazole units in 8a-8u series had a profound effect on antitumor activity. ...

Design and synthesis of novel Imidazo[2,1-b]thiazole derivatives as potent antiviral and antimycobacterial agents. KU Leuven

Elif Gürsoy, Efe Doğukan Dincel, Lieve Naesens, Nuray Ulusoy Güzeldemirci
A series of novel acyl-hydrazone (4a-d) and spirothiazolidinone (5a-d, 6a-d) derivatives of imidazo[2,1-b]thiazole were synthesized and evaluated for their antiviral and antimycobacterial activity. The antituberculosis activity was evaluated by using the Microplate Alamar Blue Assay and the antiviral activity was evaluated against diverse viruses in mammalian cell cultures. According to the biological activity studies of the compounds, 5a-c ...

Analytical techniques for metabolomic studies Vrije Universiteit Brussel

Karen Segers, Sven Declerck, Debby Mangelings, Yvan Vander Heyden, Ann Van Eeckhaut

Metabolomics is the comprehensive study of small-molecule metabolites. Obtaining a wide coverage of the metabolome is challenging because of the broad range of physicochemical properties of the small molecules. To study the compounds of interest spectroscopic (NMR), spectrometric (MS) and separation techniques (LC, GC, supercritical fluid chromatography, CE) are used. The choice for a given technique is influenced by the sample matrix, the ...

Integrating Drug- and Formulation-Related Properties With Gastrointestinal Tract Variability Using a Product-Specific Particle Size Approach: Case Example Ibuprofen KU Leuven

Rodrigo Cristofoletti, Bart Hens, Nikunjkumar Patel, Valvanera Vozmediano Esteban, Stephan Schmidt, Jennifer Dressman
In the present study, an in vitro-in vivo extrapolation of dissolution integrated to a physiologically based pharmacokinetics modeling approach, considering a product-specific particle size distribution and a self-buffering effect of the drug, is introduced and appears to be a promising translational modeling strategy to support drug product development, manufacturing changes and setting clinically relevant specifications for immediate release ...