A spirooxazine dye has been doped in poly(methyl methacrylate) and ethyl cellulose nanoparticles by emulsion-solvent evaporation method. Tinuvin 144 hindered amine light stabilizer with an antioxidant moiety was selected as an efficient photostabilizer for improving the fatigue resistance of the...
Electrochemical carboxylation of benzylic carbonates was successfully performed as an alternative method for the synthesis of phenylacetic acids by using a one-compartment cell equipped with a Pt plate cathode and an Mg rod anode in CH3CN to afford the corresponding phenylacetic acids in good yi...
Panipenem/betamipron (Carbenin), a parenteral carbapenem antibiotic, is used for the treatment of severe and intractable bacterial infections caused by gram-positive and gram-negative bacteria. Because 30% of panipenem and most of the betamipron are excreted in the urine in an unchanged form, re...
d-Ribono-1,4-lactone was treated with ethylamine in DMF to afford N-ethyl-d-ribonamide 8a in quantitative yield. Using this reaction procedure, N-butyl, N-hexyl, N-dodecyl, N-benzyl, N-(3-methyl-pyridinyl)-, N-(2-hydroxy-ethyl)-, and N-(2-cyano-ethyl)-d-ribonamides 8b–h were obtained in quantit...
A new one-step procedure for the synthesis of monoalkylated calix[4]arenes is presented. Reaction of calix[4]arene 1a or 1b with 1.2 equivalent of a weak base (K2CO3 in MeCN or CsF in DMF) and excess of alkylating agent affords the monoalkylated calix[4]arenes in moderate to good yields.
Two new polymers containing pendant calix[4]arene units with nitrile functionalities at their lower rim have been synthesized via radical initiated reactions involving a vinylic monomer 6 {5,11,17,23-tetra-tert-butyl-25,26,27-tris(cyanomethoxy)-28-(2-acryloyloxy) ethoxycalix[4]arene} and with st...
Enthalpies of solution of 2,8,14,20-tetramethyl-4,6,10,12,16,18,22,24-octahydroxyresorci[4]arene in methanol, ethanol and propanol as a function of molal concentration at (288.15, 298.15 and 308.15) K were measured calorimetrically. The enthalpies of solvation were estimated. Using propanol as t...
The diverse biological activities of γ-hydroxyalkenal phospholipids and their involvement in disease are the subject of intense study. Phospholipid aldehydes, such as the 4-hydroxy-7-oxohept-5-enoic acid ester of 2-lyso-phosphatidylcholine (HOHA-PC), the 5-hydroxy-8-oxo-6-octenoic acid ester of...
The synthesis, the physiochemical and the breast cancer inhibiting properties of [meso- and rac-1,2-bis(4-fluorophenyl)ethylenediamine]chloro[sulfinylbis(methane)-S]platinum(II) chlorides (meso- and rac-4F-PtCl(DMSO)) are described. Rac-4F-PtCl(DMSO) surpasses the standard carboplatin in its eff...
The synthesis and structural characterization of mammary tumor-inhibiting, diastereomeric [1,2-bis(2,6-dihalo-3-hydroxyphenyl)ethylenediamine]platinum(II) complexes with 2,6-Cl2, 2-F, 6-Cl, 2-Cl, 6-F and 2,6-F2 substituents (1-PtSO4 to 4-PtSO4) are described. The related 1,2-diphenylethylenediam...
The synthesis of the diastereomeric 1,2-bis(2-,3- and 4-fluorophenyl)ethylenediamines 4–6, 10–12 from meso-1,2-bis(2-hydroxyphenyl)ethylenediamine and 2-, 3- and 4-fluorobenzaldehyde by a diaza-Cope-rearrangement and their conversion into the [1,2-bis(2-, 3- and 4-fluorophenyl)ethylenediamine]...
A controlled trial of the use of either 0·05 per cent chlorhexidine for bathing burn wounds or the topical application of a cream containing cerium nitrate and silver sulphadiazine showed that the cerium-flamazine cream significantly reduced the degree of Pseudomonas aeruginosa contamination of...
This review summarizes advances in the chemistry of acridines concerning properties, isolation of natural products possessing the acridine ring as a partial structure, new structures of biologically active acridines, and applications of acridines as fluorescent, chemiluminescent, or sensor mater...
The design and discovery of JDTic as a potent and selective kappa opioid receptor antagonist used the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine pharmacophore as the lead structure. In order to determine if the 3-methyl or 4-methyl groups were necessary in JDTic and JDTic ana...
A series of novel N-arylmethyl substituted piperidine-linked aniline derivatives were designed, synthesized and evaluated for their anti-HIV activity in MT-4 cells. All the new compounds showed moderate to potent activities against wild-type (wt) HIV-1 with an EC50 range from 0.022 to 2.1 μM. A...
Acquired immunodeficiency syndrome (AIDS) caused by the human immunodeficiency virus (HIV) is one of the most destructive epidemics in history. Inhibitors of HIV enzymes are the main targets to develop drugs against that disease. Nonnucleoside reverse transcriptase inhibitors of HIV-1 (NNRTIs) a...
Molecular modeling studies were carried out on a series of benzimidazole and imidazo[1,2-a]pyridines as Plk1 inhibitors. Based on the pharmacophore model, we obtained a five-featured hypothesis AADRR, with two hydrogen bond acceptors, one hydrogen bond donor and two aromatic rings. An atom-based...
A library of eighty-six assorted benzimidazole derivatives was screened for antiviral activity against a panel of ten RNA and DNA viruses.Fifty-two of them displayed different levels of activity against one or more viruses, among which CVB-5, RSV, BVDV and Sb-1 were the most frequently affected....
A series of benzimidazole–oxindole conjugates were synthesized and evaluated for their cytotoxic activity. The cytotoxicity assay results suggest that conjugates 5c and 5p exhibit promising cytotoxicity against human breast cancer cell line (MCF-7). The Cell cycle analysis revealed that these c...
IntroductionRadiolabeled fatty acids are valuable metabolic tracers for PET imaging. Carbon-11 is widely used in clinical PET studies due to the prevalence of facile techniques enabling the incorporation of [11C]CO2 and [11C]CH3 into molecules and a short half-life (20.4 min) that translates int...
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