4509-90-4Relevant academic research and scientific papers
Synthesis and biological activity of homologous piperidine-containing alkyl glycerolipids
Romanova,Serebrennikova,Shtil
, p. 641 - 644 (2009)
The paper provides the synthesis of new phosphorless glycerolipids with an ether bond that contain heterocyclic bases in the polar domain. The physico-chemical characteristics and biological activity of the prepared compounds were studied.
Iron(II) complex of octopus-porphyrin with a covalently linked proximal imidazole; self-assembly and O2-coordination in aqueous media
Komatsu,Hayakawa,Yanagimoto,Kobayakawa,Nakagawa,Tsuchida
, p. 1703 - 1707 (2001)
The iron complex of tetrakis[2,6-di(alkanoyloxy)phenyl]porphyrin derivative with seven phosphocholine head groups and an N-alkylimidazole side-chain as the proximal base (octopus-porphyrin) has been synthesized. The ferrous complex (7b) was easily dispersed in water to provide a stable colloid. Transmission electron microscopy and scanning force microscopy of the evaporated solution showed spherical micelles with a diameter of 8 nm, which probably consists of a dimer of 7b. These micellar aggregates could reversibly coordinate O2 at 25 °C and the O2-binding parameters are also given.
Formal synthesis of (+)-tashiromine and study toward the total synthesis of (+)-stemoamide
Chen, Yue-Jie,Bao, Rui-Yang,Zhang, Xiao-Dong,Tang, Ye-Feng
, p. 953 - 956 (2013)
An efficient formal synthesis of (+)-tashiromine was achieved by employing an intermolecular asymmetric Mannich-type reaction as the key step. Concurrently, a novel approach toward the total synthesis of (+)-stemoamide through dyotropic rearrangement of 3,4-cis-β-lactone was also explored.
β-Cyclodextrin Host-Guest Complexes Probed under Thermodynamic Equilibrium: Thermodynamics and AFM Force Spectroscopy
Auletta, Tommaso,De Jong, Menno R.,Mulder, Alart,Van Veggel, Frank C. J. M.,Huskens, Jurriaan,Reinhoudt, David N.,Zou, Shan,Zapotoczny, Szczepan,Schoenherr, Holger,Vancso, G. Julius,Kuipers, Laurens
, p. 1577 - 1584 (2004)
The rupture forces of individual host-guest complexes between β-cyclodextrin (β-CD) heptathioether monolayers on Au(111) and several surface-confined guests were measured in aqueous medium by single molecule force spectroscopy using an atomic force microscope, Anilyl, toluidyl, tert-butylphenyl, and adamantylthiolss (0.2-1%) were immobilized in mixed monolayers with 2-mercaptoethanol on gold-coated AFM tips, For all guests and for all surface coverages, the force-displacement curves measured between the functionalized tips and monolayers of β-CD exhibited single, as well as multiple, pull-off events, The histograms of the pull-off forces showed several maxima at equidistant forces, with force quanta characteristic for each guest of 39 ± 15, 45 ± 15, 89 ± 15, and 102 ± 15 pN, respectively. These force quanta were independent of the loading rate, indicating that, because of the fast complexation/decomplexation kinetics, the rupture forces were probed under thermodynamic equilibrium. The force values followed the same trend as the free binding energy ΔG° measured for model guest compounds in solution or on β-CD monolayers, as determined by microcalorimetry and surface plasmon resonance measurements, respectively, A descriptive model was developed to correlate quantitatively the pull-off force values with the ΔG° of the complexes, based on the evaluation of the energy potential landscape of tip-surface interaction.
Brassinosteroid-BODIPY conjugates: Design, synthesis, and properties
Malachowska-Ugarte, Magdalena,Sperduto, Claudio,Ermolovich, Yuri V.,Sauchuk, Alina L.,Jurá?ek, Michal,Litvinovskaya, Raisa P.,Straltsova, Darya,Smolich, Igor,Zhabinskii, Vladimir N.,Dra?ar, Pavel,Demidchik, Vadim,Khripach, Vladimir A.
, p. 53 - 59 (2015)
Three BS-BODIPY (brassinosteroids-4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) conjugates were synthesized and their fluorescent and immunological properties were investigated. Two of the conjugates, having present all the functional groups characteristic of BS, were shown to be potentially useful as biological probes to study involvement of BS into physiological processes in living cells.
Nucleic acid-induced aggregation and pyrene excimer formation
Zhang, Ruixing,Tang, Dan,Lu, Ping,Yang, Xiangyu,Liao, Dongli,Zhang, Yujing,Zhang, Mingjun,Yu, Cong,Yam, Vivian W. W.
, p. 4302 - 4305 (2009)
Nucleic acid was found to induce the aggregation of the positively charged pyrene probe (compound 1); as a result, strong pyrene excimer emission was observed. The Intensity of the excimer emission was dependent on the concentration of the pyrene probe and the oligonucleotide length, sequence, and concentration. These results suggest a new strategy for label-free nucleic acid-based biosensing applications.
Synthesis of novel C-2- or C-15-labeled BODIPY—estrone conjugates
Bacsa, Ildikó,Konc, Csilla,Orosz, Anna Boglárka,Kecskeméti, Gábor,Rigó, Réka,zvegy-Laczka, Csilla,Mernyák, Erzsébet
, (2018)
Novel BODIPY–estrone conjugates were synthesized via Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC). Estrone-alkynes or an estrone-azide as starting compounds were synthesized via Michael addition or Sonogashira reaction as key steps. Fluorescent dyes based on BODIPY-core were provided by azide or alkyne functional groups. Fluorescent labeling of estrone was efficiently achieved at the C-2 or C-15 position. The newly-elaborated coupling procedures might have a broad applicability in the synthesis of fluorescent-labeled estrone conjugates suitable for biological assays.
Oseltamivir PROTAC compound as well as preparation method and application thereof in anti-influenza virus medicines
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Paragraph 0048-0051, (2021/04/03)
The invention discloses an oseltamivir PROTAC compound as well as a preparation method and application thereof in anti-influenza virus medicines, and belongs to the technical field of medicines. The oseltamivir PROTAC compound is shown as a general formula (I) or (II), and in the general formula, E3 ligase is a VHL or CRBN ligand, and Linker is a linking group. The compound provided by the invention can effectively degrade influenza virus neuraminidase so as to exert the activity of inhibiting influenza virus replication, not only has inhibitory activity on wild influenza viruses, but also hasa very good inhibitory effect on oseltamivir drug-resistant strains, and has low toxicity to cells. The compound or the pharmacologically or physiologically acceptable salt thereof can be used for preparing anti-influenza virus medicines.
PDE4 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC APPLICATIONS
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Paragraph 0331, (2021/06/22)
Provided herein are phosphodiesterase 4 (PDE4) inhibitors, e.g., a compound of Formula (I) or (II), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a disease, disorder, or condition associated with PDE4 malfunction.
Gemfibrozil derivatives as activators of soluble guanylyl cyclase – A structure-activity study
Baker, Hannah,Ferreira, Liam D.,Gayler, Kevin M.,Kane, Robert R.,Karunananthan, Johann W.,Kostyo, Jessica H.,Martin, Emil,Mattke, Jordan,Nguyen, Harold,Plunk, Michael A.,Quintana, Jeremy M.,Sharina, Iraida,Shuda, Mina,Stinchcomb, Alexandra L.
, (2021/08/09)
Previous studies demonstrated that anti-hyperlipidemic drug gemfibrozil acts as NO- and heme-independent activator of NO receptor soluble guanylyl cyclase. A series of new gemfibrozil derivatives were synthesized and evaluated for sGC activation. The structure-activity relationship study identified the positions in gemfibrozil's scaffold that are detrimental for sGC activation and those that are amendable for optimizing modifications. Compared with gemfibrozil, compounds 7c and 15b were more potent activators of cGMP-forming activity of purified sGC and exhibited enhanced relaxation of preconstricted mouse thoracic aorta rings. These studies established the overall framework needed for futher improvement of sGC activators based on gemfibrozil scaffold.
