Search results for "Biological activity"
showing 10 items of 465 documents
Cyclic Analogs of Desferrioxamine E Siderophore for 68Ga Nuclear Imaging: Coordination Chemistry and Biological Activity in Staphylococcus aureus
2021
As multidrug-resistant bacteria are an emerging problem and threat to humanity, novel strategies for treatment and diagnostics are actively sought. We aim to utilize siderophores, iron-specific strong chelating agents produced by microbes, as gallium ion carriers for diagnosis, applying that Fe(III) can be successfully replaced by Ga(III) without losing biological properties of the investigated complex, which allows molecular imaging by positron emission tomography (PET). Here, we report synthesis, full solution chemistry, thermodynamic characterization, and the preliminary biological evaluation of biomimetic derivatives (FOX) of desferrioxamine E (FOXE) siderophore, radiolabeled with 68Ga …
Plant-growth-regulating phosphono peptides
1990
Phosphono peptides exhibited plant‐growth‐regulating activity when tested on Lepidium sativum and Cucumis sativus. The studies have provided evidence that the mechanism of action of these compounds may involve the uptake of the phosphono peptides into the plant, intracellular hydrolysis of the peptide bond and release of the P‐terminal aminoalkylphosphonic acid. This acid or its metabolite is then probably responsible for the observed physiological effect.
Synthesis and antiproliferative activity of 2'-O-allyl-1-beta-D-arabynofuranosyl-uracil, -cytosine and -adenine
1997
Abstract With the aim to design potential inhibitors of ribonucleotide reductase (RR), 2′-O-allyl-β-D-arabinofuranosyl-uracil ( 4 ), -cytosine ( 7 ) and -adenosine ( 10 ) were prepared and evaluated for their cytostatic activity against Molt4/C8, CEM and L1210 cell lines. Although our preliminary data do not allow to assess if RR is the intracellular target, the results point to differences in the (anti)metabolic behavior of these compounds. This study also offers a general synthesis of 2′-O-allyl-β-D-arabinofuranosyl nucleosides for potential applications in the preparation of 2′-O-allyl-β-D-oligoarabino nucleotides.
Biological Activities of Natural Sesquiterpene Lactones and the Effect of Synthetic Sesquiterpene Derivatives on Insect Juvenile Hormone Biosynthesis
1998
Three natural sesquiterpene lactones have been assayed for their biological activity on locust (Locusta migratoria) nymphs. Since results obtained in vivo pointed to disruptions on juvenile hormone (JH)-regulated physiology, we tested the sesquiterpene lactones and a family of synthetic sesquiterpene derivatives for their ability to disturb the rate of JH biosynthesis by locust corpora allata (CA) in vitro. All the active compounds in vitro share a basic sesquiterpene double-ring structure as well as substituents with different chemical complexities. Compounds that shared an eudesmane base with different oxidation states on C3 and C12 carbon atoms were tested as JH biosynthesis inhibitors. …
Novel Stilbene-Based Antileukemic Agents Active in P-Glycoprotein Expressing and Apoptosis-Resistant Acute Leukaemia Cell Lines.
2005
Abstract The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds and in accordance with Evans’ definition it can be considered as a privileged structure. One of the most relevant and studied stilbenes is Resveratrol, a phytoalexin present in grapes, endowed with chemopreventive and chemotherapeutic properties and able to induce apoptosis in different cancer cell lines. Since reduced apoptosis has been implicated in the development and progression of malignant tumors and in the occurrence of chemoresistant phenotypes, resveratrol-induced apoptosis might therefore contribute to its antitumor activity. However, resveratrol is a not potent cy…
Rollimembrin, a novel acetogenin inhibitor of mammalian mitochondrial complex I
1997
Abstract Rollimembrin (3), is a new adjacent bis-tetrahydrofuranic acetogenin with a scarce relative configuration, threo/cis/threo/cis/erythro, isolated from Rollinia membranacea seeds. The mechanism of cytotoxic activity, determined by NADH-oxidase experiments, establish that rollimembrin (3) is the most potent inhibitor of mammalian mitochondrial complex I.
Saponins as immunoadjuvants and immunostimulants
1999
Saponins are either triterpene or steroid glycosides widely distributed in the plant and animal kingdom and include a large number of biologically active compounds. Most of them have surface-active and cholesterol-binding properties.
Entzündungshemmende wirkstoffe. XI. Ringschlußreaktion an 5-phenyl-2-thiobiuret
1988
Die Umsetzung von 5-Phenyl-2-thiobiuret (1) mil α-Chlorcarbonylverbindungen 2 fuhrt zu den N-Phenyl-N′-(2-thiazolyl)harnstoffen (3). Unter den neuen Verbindungen finden sich besonders die entzundungshemmende, anthelminthische und trichomonazide Wirksamkeit stark ausgepragt. The reaction of 5-phenyl-2-thiobiuret (1) with α-chlorocarbonyl compounds 2 leads to the structure type of N-phenyl-N1-(thiazolyl)urea (3). The new compounds exhibit particularly antiinflammatory, anthelminthic, and trichomonacidal activity.
Structure and properties of pharmacologically active polymers
1975
Although the concept of using pharmacologically active macromolecular compounds as drugs is still regarded with much skepticism for both theoretical and practical reasons, interest in this field has grown in recent years because of the opportunity to take advantage of the specific properties of polymeric materials. For low molecular weight drugs, changes in structure often lead to a loss of specific activity. On the other hand, the properties of macromolecular drugs depend on the structure of the polymer used and this can be varied over a wide range by the incorporation of comonomer units, by the application of polymer-analogous reactions, or by related structural changes. A new model is pr…
H2-Antihistaminika, 32. Mitt. Synthese und H2-antagonistische Wirkung von N-[3-(3-Piperidino-methyl-phenoxy)propyl]-1.3.4-oxadiazol-2-aminen
1986
Es wird uber die Synthese und H2-antagonistische Wirksamkeit von N-[3-(3-Piperidinomethyl-phenoxy)-propyl]-1.3.4-oxadiazol-2-amin und dessen 5-substituierte Derivate berichtet. H2-Antihistaminics, XXXII: Synthesis and H2-Antagonistic Activity of N-[3-(3-(Piperidinomethyl)phenoxy)propyl]- 1.3.4-oxadiazol-2-amines The synthesis and H2-antagonistic activity of N-[3-(3-(piperidinomethyl)phenoxy)propyl]-l.3.4-oxadiazol-2-amine and its 5-substituted derivatives are reported.