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Università della Svizzera italiana

Isonitrile-based multicomponent synthesis of β-amino boronic acids as β-lactamase inhibitors

Bassini, Emanuele ; Gazzotti, Stefano ; Sannio, Filomena ; Lo Presti, Leonardo ; Sgrignani, Jacopo ; Docquier, Jean-Denis ; Grazioso, Giovanni ; Silvani, Alessandra

In: Antibiotics, 2020, vol. 9, no. 5, p. 21 p

The application of various isonitrile-based multicomponent reactions to protected (2-oxoethyl)boronic acid (as the carbonyl component) is described. The Ugi reaction, both in the four components and in the four centers–three components versions, and the van Leusen reaction, proved effective at providing small libraries of MIDA-protected β-aminoboronic acids. The corresponding free...

Università della Svizzera italiana

Multi-targeting bioactive compounds extracted from essential oils as kinase inhibitors

Maruca, Annalisa ; Lanzillotta, Delia ; Rocca, Roberta ; Lupia, Antonio ; Costa, Giosuè ; Catalano, Raffaella ; Moraca, Federica ; Gaudio, Eugenio ; Ortuso, Francesco ; Artese, Anna ; Trapasso, Francesco ; Alcaro, Stefano

In: Molecules, 2020, vol. 25, no. 9, p. 14 p

Essential oils (EOs) are popular in aromatherapy, a branch of alternative medicine that claims their curative effects. Moreover, several studies reported EOs as potential anti- cancer agents by inducing apoptosis in different cancer cell models. In this study, we have considered EOs as a potential resource of new kinase inhibitors with a polypharmacological profile. On the other hand,...

Università della Svizzera italiana

How computational chemistry and drug delivery techniques can support the development of new anticancer drugs

Garofalo, Mariangela ; Grazioso, Giovanni ; Cavalli, Andrea ; Sgrignani, Jacopo

In: Molecules, 2020, vol. 25, no. 7, p. 22 p

The early and late development of new anticancer drugs, small molecules or peptides can be slowed down by some issues such as poor selectivity for the target or poor ADME properties. Computer-aided drug design (CADD) and target drug delivery (TDD) techniques, although apparently far from each other, are two research fields that can give a significant contribution to overcome these problems....

Université de Fribourg

In vitro antitubercular activity of extract and constituents from the stem bark of Disthemonanthus benthamianus

Evina, Jean Noel ; Ngono Bikobo, Dominique Serge ; Zintchem, Auguste Abouem A. ; Mbabi Nyemeck II, Norbert ; Moni Ndedi, Esther Del Florence ; Betote Diboué, Patrick Hervé ; Nyegue, Maximilienne Ascension ; Atchadé, Alex de Théodore ; Pegnyemb, Dieudonné Emmanuel ; Koert, Ulrich ; Bochet, Christian G.

In: Revista Brasileira de Farmacognosia, 2017, vol. 27, no. 6, p. 739-743

A new C-glycosylflavone, apigenin 7-methyl ether 6-C-[β-xylopyranosyl-(1→3)-β- glucopyranoside] named distemonanthoside was isolated from the stem bark of Distemonanthus benthamianus Baill., Fabaceae, along with six known compounds, sitosterol 3-O-β-d-glucopyranoside, 4-methoxygallic acid, syringic acid, quercetin, 6″- O-acetylvitexin, quercetin 3-O-β-d-glucopyranoside. The structures...

Université de Fribourg

Cytotoxic flavonoids and other constituents from the stem bark of Ochna schweinfurthiana

Ndongo, Joseph T. ; Issa, Mark E. ; Messi, Angelique N. ; Mbing, Joséphine Ngo ; Cuendet, Muriel ; Pegnyemb, Dieudonné Emmanuel ; Bochet, Christian G.

In: Natural Product Research, 2015, vol. 29, no. 17, p. 1684-1687

Seven flavonoids, hemerocallone (1), 6,7-dimethoxy-3′,4′-dimethoxyisoflavone (2), amentoflavone (4), agathisflavone (6), cupressuflavone (8), robustaflavone (9) and epicatechin (10), together with three other compounds, lithospermoside (3), β-D- fructofuranosyl-α-D-glucopyranoside (5) and 3β-O-D-glucopyranosyl-β-stigmasterol (7), were isolated from the ethyl acetate extract of the stem...

Université de Fribourg

The natural diyne-furan fatty acid EV-086 is an inhibitor of fungal delta-9 fatty acid desaturation with efficacy in a model of skin dermatophytosis

Knechtle, Philipp ; Diefenbacher, Melanie ; Greve, Katrine B. V. ; Brianza, Federico ; Folly, Christophe ; Heider, Harald ; Lone, Museer A. ; Long, Lisa ; Meyer, Jean-Philippe ; Roussel, Patrick ; Ghannoum, Mahmoud A. ; Schneiter, Roger ; Sorensen, Alexandra S.

In: Antimicrobial Agents and Chemotherapy, 2013, vol. 58, no. 1, p. 455–466

Human fungal infections represent a therapeutic challenge. Although effective strategies for treatment are available, resistance is spreading, and many therapies have unacceptable side effects. A clear need for novel antifungal targets and molecules is thus emerging. Here, we present the identification and characterization of the plant-derived diyne-furan fatty acid EV-086 as a novel antifungal...

Université de Fribourg

Arginase: the emerging therapeutic target for vascular oxidative stress and inflammation

Yang, Zhihong ; Ming, Xiu-Fen

In: Frontiers in Inflammation, 2013, vol. 4, p. 149

Oxidative stress and inflammation in the vascular wall are essential mechanisms of atherosclerosis and vascular dysfunctions associated with risk factors such as metabolic diseases, aging, hypertension, etc. Evidence has been provided that activation of the vascular endothelial cells in the presence of the risk factors promotes oxidative stress and vascular inflammatory responses, leading to...

Université de Genève

Isolement de xanthones et coumarines inhibitrices de l'acétylcholinestérase, respectivement à partir de "Gentianella campestris" (L.) Börner et "Gentianella amarella" (L.) Börner ssp. "acuta" (Michx.) J.M. Gillett (Gentianaceae), et "Peucedanum ostruthium" (L.) Koch (Apiaceae)

Urbain, Aurélie ; Hostettmann, Kurt (Dir.)

Thèse de doctorat : Université de Genève, 2007 ; Sc. 3934.

Lors d'un criblage visant à détecter des extraits végétaux présentant une activité inhibitrice de l'acétylcholinestérase, trois espèces se sont révélées significativement actives; deux Gentianaceae: "Gentianella campestris" et "Gentianella amarella" ssp. "acuta", et une Apiaceae: "Peucedanum ostruthium". Les composés d'intérêt ont été isolés essentiellement par chromatographie...

Université de Genève

Suivi thérapeutique de la ciclosporine : approche analytique et pharmacogénétique

Ansermot, Nicolas ; Hochstrasser, Denis François (Dir.) ; Veuthey, Jean-Luc (Codir.)

Thèse de doctorat : Université de Genève, 2007 ; Sc. 3912.

La présente thèse aborde des aspects analytiques et pharmacogénétiques du suivi thérapeutique des immunosuppresseurs. Dans un premier temps, une méthode de dosage sanguin simultané de plusieurs immunosuppresseurs par chromatographie liquide couplée à la spectrométrie de masse a été développée et comparée avec une technique immunologique. En utilisant le même outil analytique, une...