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1.
Mini Rev Med Chem ; 21(19): 3052-3061, 2021.
Article in English | MEDLINE | ID: mdl-34137362

ABSTRACT

It is estimated that by 2040, Chronic Kidney Disease (CKD) will be the 5th main cause of global deaths. It has been suggested that hyperphosphatemia is among the main factors leading to the increased risk of death. This review focuses on potential and currently used Phosphate Binders (PB). Aluminum hydroxide is presently not recommended due to potential aluminum toxicity. Calciumcontaining phosphate binders (CCPB) can cause calcium overload, resulting in hypercalcemia and an increased risk of cardiovascular diseases. Magnesium and calcium complexes were suggested to be as effective as sevelamer in the reduction of serum phosphate, with the potential to slow down the process of calcification. However, limited studies have been conducted in this area. Although sevelamer seemed to have a positive influence on cardiovascular calcification and arterial stiffness, its influence on mortality was unclear. Sevelamer crystal accumulation in the Gastrointestinal tract (GI) can cause gastrointestinal bleeding. Lanthanum carbonate seemed to lower all-cause mortality and reduce the chance of hypercalcemia, even though a deposit in the GI tract was observed. Colestilan, like sevelamer, reduced LDL cholesterol. Sucroferric oxyhydroxide had a lower pill burden than other PBs and it seemed to reduce serum FGF-23. Ferric citrate improved parameters that are related to anemia but can cause iron overload. Bixalomer appeared to have fewer gastrointestinal side effects than sevelamer. Nano-lanthanum hydroxide and SBR759 may have an interesting future as PBs. In conclusion, the development of new PBs should also take into consideration their potential to function as protection modifiers.


Subject(s)
Hyperphosphatemia , Renal Insufficiency, Chronic , Chelating Agents/therapeutic use , Humans , Hyperphosphatemia/chemically induced , Hyperphosphatemia/drug therapy , Phosphates/therapeutic use , Renal Insufficiency, Chronic/chemically induced , Renal Insufficiency, Chronic/complications , Renal Insufficiency, Chronic/drug therapy , Sevelamer/therapeutic use
2.
Polymers (Basel) ; 12(11)2020 Nov 16.
Article in English | MEDLINE | ID: mdl-33207751

ABSTRACT

In this study, the photo-optical properties of the series of new 1H-pyrazolo[3,4-b]quinoline derivatives were investigated. Pyrazoloquinoline studies were conducted to explain the electroluminescent effect in organic LEDs. Absorption and photoluminescence spectra for the materials under consideration were examined, and quantum chemical calculations were made. Differential scanning calorimetric and thermogravimetric measurements were carried out for the manufactured materials. The phase situation of the materials was determined, and glassy transitions were detected for three of the investigated materials. Degradation temperatures were obtained. Single-layer luminescent diodes based on the ITO/PEDOT:PSS/active layer/Al scheme were fabricated. Current-voltage and brightness-voltage characteristics of the diodes were determined, ignition voltage was calculated, and electroluminescence types were determined.

3.
Eur Biophys J ; 48(4): 371-381, 2019 May.
Article in English | MEDLINE | ID: mdl-31004192

ABSTRACT

Although much research has been performed on DNA complexes carrying long alkyl chains (C10, C16, and C18), there is no information about physicochemical characterization of synthesized composites with allyl imidazole-based ionic liquids and quaternary ammonium salts with n-butyl chains. Here, complexes were synthesized by ion-exchange reactions between sonicated DNA and three ionic liquids (ILs) formed from two imidazole-based compounds, 1-allyl-3-methylimidazolium bromide (Amim) or 1-butyl-3-methylimidazolium bromide (Bmim), and from the quaternary ammonium salt tetra-n-butylammonium bromide (TBAB). Signals in UV-Vis, IR, and CD spectra indicating inclusion of small molecules into the DNA structure confirmed the formation of DNA complexes. Both IR and CD spectra indicated that the B-form conformation of the DNA did not change after the formation of the complexes. Similarly, X-ray diffraction patterns revealed that the formation of IL-DNA complexes did not change the structure of native B-form DNA. Molecular weight (Mw) and radii of gyration (Rg) values of IL-DNA complex chains, established by high-performance size exclusion chromatography coupled with multiangle-laser light-scattering with a differential refractive index detector, were significantly lower than those values found for native DNA molecules due to DNA fragmentation by sonication during complex formation and the direct effects of the IL on the DNA. Scanning electron microscopy images indicate the formation of nanofibres in DNA-Amim and DNA-Bmim complexes, whereas the formation of nanowires was found in samples of DNA-TBAB complexes. Changes in optical properties confirmed by UV and photoluminescence make DNA-IL complexes potential candidates for biosensor application.


Subject(s)
DNA/chemistry , Surface-Active Agents/chemistry , Chemical Phenomena , Ionic Liquids/chemistry
4.
J Fluoresc ; 21(1): 375-83, 2011 Jan.
Article in English | MEDLINE | ID: mdl-20890644

ABSTRACT

A novel fluorescent dye bis-(pyridin-2-yl-methyl)-(1,3,4-triphenyl-1H-pyrazolo[3,4-b]quinolin-6-ylmethyl)-amine (P1) has been synthesized and investigated by means of steady state and time-resolved fluorescence techniques. This compound acts as sensor for fluorescence detection of small inorganic cations (lithium, sodium, barium, magnesium, calcium, and zinc) in highly polar solvents such as acetonitrile. The mechanism which allows application of this compound as sensor is an electron transfer from the electron-donative part of molecule (amine) to the acceptor part (pyrazoloquinoline derivative), which is retarded upon complexation of the electro-donative part by inorganic cations. The binding constants are strongly dependent on the charge density of the analyzed cations. The 2/1 complexes of P1 with Zn(++) and Mg(++) cations posses large binding constants. Moreover, in the presence of these cations a significant bathochromic shift of fluorescence is observed. The most probable explanation of such behaviour is the formation of intramolecular excimer. This is partially supported by the quantum chemical calculations.

5.
Bioorg Med Chem ; 16(1): 511-7, 2008 Jan 01.
Article in English | MEDLINE | ID: mdl-17904371

ABSTRACT

This paper describes the synthesis and the antiviral activities of dimeric compounds derived from homo and asymmetric combinations of N-1 propynyloxymethyl analogues 1a,b of MKC-442, an N-1 4-iodobenzyloxymethyl analogue of TNK-651 5, potent contraceptive norgestrel and AZT. They were obtained by Sonogashira reaction, 'click' chemistry or Pd-catalyzed oxidative coupling. The iodo precursor 5 turned out as a potent compound against wild type and mutated HIV-1 virus. All dimeric compounds showed lower activity against HIV-1 than MKC-442, except the asymmetric dimer of AZT and 1a which showed an activity comparable to MKC-442.


Subject(s)
Anti-HIV Agents/chemical synthesis , HIV-1/drug effects , Anti-HIV Agents/pharmacology , Dimerization , HIV-1/genetics , Humans , Mutation , Pyrimidines/chemistry , Pyrimidines/pharmacology , Uracil/analogs & derivatives , Uracil/chemistry , Uracil/pharmacology , Zidovudine/chemistry , Zidovudine/pharmacology
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