- Base-Catalyzed, Solvent-Free Synthesis of Rigid V-Shaped Epoxydibenzo[b,f][1,5]diazocines
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A novel method for the synthesis of epoxydibenzo[b,f][1,5]diazocines exhibiting a V-shaped molecular architecture is reported. The unique approach is based on unprecedented base-catalyzed, solvent-free autocondensation and cross-condensation of fluorinate
- Bisek, Bartosz,Górecki, Marcin,Michalak, Micha?,Nowacki, Micha?
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- Multifunctional photodegradable polymers for reactive micropatterns
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We report the first example of realizing the multifunctionalization of photodegradable polymers for the preparation of reactive micropatterns. Three o-nitrobenzaldehyde monomers (M1, M2, and M3) with allyl, propargyl, and epoxy groups were synthesized in
- Li, Lei,Deng, Xin-Xing,Li, Zi-Long,Du, Fu-Sheng,Li, Zi-Chen
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- Synthesis and biological evaluation of novel quinazoline-triazole hybrid compounds with potential use in Alzheimer's disease
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A library of twelve quinazoline-triazole hybrid compounds were designed, synthesized and evaluated as a novel class of acetylcholinesterase inhibitors to treat Alzheimer's disease (AD). The biological assay results demonstrated the ability of several hybrid compounds to inhibit AChE enzyme (IC50 range = 0.2–83.9 μM). To understand the high potential activity of these compounds, molecular docking simulations were performed to get better insights into the mechanism of binding of quinazoline-triazole hybrid compounds. As expected, compounds 8a and 9a-b bind to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active site of AChE enzyme, which implicates that these compounds could act as dual binding site inhibitors. These compounds were not cytotoxic and they also displayed appropriated physicochemical as well as pharmacokinetic profile to be developed as novel anti-AD drug candidates.
- Dang Thi, Tuyet Anh,Le-Nhat-Thuy, Giang,Nguyen Hoang, Sa,Nguyen Thi, Huong,Nguyen Thi, Nga,Nguyen Thi, Thu Ha,Nguyen, Tuyen Van,Pham-The, Hai
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supporting information
(2020/07/23)
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- Synergic effect on oxygen reduction reaction of strapped iron porphyrins polymerized around carbon nanotubes
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In the context of the development of new bio-inspired catalysts, MN4 complexes exhibit a great potential for small molecule activation. In particular, metallated porphyrins and phthalocyanines combined with carbon nanotubes have been tested for the oxygen reduction reaction in electrocatalytic systems, and these nanotube/MN4 hybrids have demonstrated promising properties. Here, a series of hybrid materials made of multi-walled carbon nanotubes (MWNTs) coated with strapped porphyrins have been fabricated. Iron porphyrin derivatives were polymerized around the nanotubes via Hay coupling and the resulting materials were fully characterized. Two porphyrins were probed; both were strapped with the same skeleton and they differed only in the presence or absence of overhung carboxylic acids. In the porphyrin, the carboxylic acid group could possibly act as a proton relay between the medium and the catalyst. Although the presence of the carboxylic acid groups (acting as intramolecular proton relays) did not exhibit a significant influence on the catalytic properties, the combination of both components-the MWNTs and porphyrin-led to a better catalytic activity than those of the nanotubes or the porphyrins taken separately. The synergic affect is due to the MWNTs which ensure the availability of electrons to the porphyrin catalysts and allow the ORR to occur via the 4-electron pathway, avoiding the production of hydrogen peroxide.
- Hanana, Manel,Arcostanzo, Hélène,Das, Pradip K.,Bouget, Morgane,Le Gac, Stéphane,Okuno, Hanako,Cornut, Renaud,Jousselme, Bruno,Dorcet, Vincent,Boitrel, Bernard,Campidelli, Stéphane
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supporting information
p. 19749 - 19754
(2018/12/13)
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- Photo-triggered release of caged camptothecin prodrugs from dually responsive shell cross-linked micelles
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We report on the fabrication of dynamic covalent shell cross-linked (SCL) micelles with hydrophobic cores conjugated with photocaged chemotherapeutic drugs and coronas functionalized with ligands for tumor cell targeting. Two types of amphiphilic diblock
- Hu, Xianglong,Tian, Jie,Liu, Tao,Zhang, Guoying,Liu, Shiyong
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p. 6243 - 6256
(2013/09/02)
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- L-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: A novel series of potent calcium-sensing receptor antagonists
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Parathyroid hormone (PTH) is an effective bone anabolic agent. However, only when administered by daily sc injections exposure of short duration is achieved, a prerequisite for an anabolic response. Instead of applying exogenous PTH, mobilization of endogenous stores of the hormone can be envisaged. The secretion of PTH stored in the parathyroid glands is mediated by a calcium sensing receptor (CaSR) a GPCR localized at the cell surface. Antagonists of CaSR (calcilytics) mimic a state of hypocalcaemia and stimulate PTH release to the bloodstream. Screening of the internal compound collection for inhibition of CaSR signaling function afforded 2a. In vitro potency could be improved > 1000 fold by optimization of its chemical structure. The binding mode of our compounds was predicted based on molecular modeling and confirmed by testing with mutated receptors. While the compounds readily induced PTH release after iv application a special formulation was needed for oral activity. The required profile was achieved by using microemulsions. Excellent PK/PD correlation was found in rats and dogs. High levels of PTH were reached in plasma within minutes which reverted to baseline in about 1-2 h in both species.
- Widler, Leo,Altmann, Eva,Beerli, René,Breitenstein, Werner,Bouhelal, Rochdi,Buhl, Thomas,Gamse, Rainer,Gerspacher, Marc,Halleux, Christine,John, Markus R.,Lehmann, Hansjoerg,Kalb, Oskar,Kneissel, Michaela,Missbach, Martin,Müller, Irene R.,Reidemeister, Sibylle,Renaud, Johanne,Taillardat, Agnes,Tommasi, Ruben,Weiler, Sven,Wolf, Romain M.,Seuwen, Klaus
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supporting information; experimental part
p. 2250 - 2263
(2010/08/21)
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- ARYL-QUINAZOLINE/ARYL-2AMINO-PHENYL METHANONE DERIVATIVES
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A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
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Page/Page column 27-28
(2008/06/13)
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