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    Wyświetlanie 1-7 z 7
    Tytuł:
    Anti-tumor agents: Design, Synthesis, and Biological study of N-Substituted-7-hydroxy-1-azacoumarin-3-carboxamide derivatives as potent cytotoxic agents
    Autorzy:
    Bakare, Safyah B.
    Powiązania:
    https://bibliotekanauki.pl/articles/1849341.pdf
    Data publikacji:
    2021
    Wydawca:
    Zachodniopomorski Uniwersytet Technologiczny w Szczecinie. Wydawnictwo Uczelniane ZUT w Szczecinie
    Tematy:
    azacoumarin-3-carboxamide
    cytotoxicity
    1H
    13C-NMR
    spectraMCF-7
    Opis:
    Synthesis of ethyl 7-hydroxy-1-azacoumarin-3-carboxylate (3) was developed using ethyl-7-hydroxy coumarin-3-carboxylate and ammonium solution as the key synthons. Condensation of ethyl 7-hydroxy-1-azacoumarin-3-carboxylate with ammonium acetate and aniline to give N-substituted-7-hydroxy-1-azacoumarin-3-carboxamides (7-Hydroxy -1-azacoumarin-3-carboxamide (4) and N-phenyl 7-Hydroxy-1-azacoumarin-3-carboxamide (5)). Bromo derivative (N-phenyl 6, 8-dibromo-7-hydroxy-1-azacoumarin-3-carboxamide (6)) was obtained from halogenation of compound N-phenyl 7-Hydroxy-1-azacoumarin-3-carboxamide (5) with bromine in glacial acetic acid. N-phenyl-2,5-diacetoxy-6, 8-disubstituted-Quinoline-3-carboxamides (N-phenyl 2,7-diacetoxy-Quinoline-3-carboxamide (7) and N-phenyl 2,7-diacetoxy-6,8-dibromo-Quinoline-3-carboxamide (8)) were prepared via the acetylation of compounds 5 and 6 with acetic anhydride. Five compounds 4–8 were evaluated in vitro against more than one human tumor cell lines. Among the selected compounds, 6 showed the best in vitro cytotoxicity against the human cancer cell line; MCF-7 (with IC50 = 10.12 μM). In addition, cell cycle analysis of compound 6 demonstrated cell cycle arrest at G2/M phase and Pre-G1 apoptosis.
    Źródło:
    Polish Journal of Chemical Technology; 2021, 23, 1; 53-59
    1509-8117
    1899-4741
    Pojawia się w:
    Polish Journal of Chemical Technology
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Effects of 1-methylnicotinamide and its metabolite N-methyl-2-pyridone-5-carboxamide on streptozotocin-induced toxicity in murine insulinoma MIN6 cell line
    Autorzy:
    Przygodzki, Tomasz
    Slominska, Ewa
    Polakowska, Ewa
    Mlynarski, Wojciech
    Watala, Cezary
    Powiązania:
    https://bibliotekanauki.pl/articles/1039953.pdf
    Data publikacji:
    2011
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    nucleotide pool
    streptozotocine
    1-methylnicotinamide
    N-methyl-2-pyridone-5-carboxamide
    Opis:
    1-methylnicotinamide (MNA) is a primary metabolite of nicotinamide. In recent years several activities of MNA have been described, such as anti-inflammatory activity in skin diseases, induction of prostacyclin synthesis via COX-2, aortal endothelium protection in diabetes and hypertriglyceridaemia and increased survival rate of diabetic rats. 1-methylnicotinamide was also suggested to protect pancreatic cells from streptozotocin in vivo. Streptozotocin toxicity is known to be mediated by poly-ADP-ribose polymerase. Nicotinamide and its derivatives have been shown to ameliorate poly-ADP-ribose polymerase-dependent nucleotide pool reduction. We aimed to verify if 1-methylnicotinamide and its metabolite, N-methyl-2-pyridone-5-carboxamide, can protect insulinoma cells from streptozotocin-induced toxicity. We found that N-methyl-2-pyridone-5-carboxamide, but not 1-methylnicotinamide, restores the pool of ATP and NAD+ in streptozotocin-treated cells, but neither compound improved the cell viability. We conclude that inhibition of poly-ADP-ribose polymerase-dependent nucleotide pool reduction may not be sufficient to protect cells from streptozotocin toxicity.
    Źródło:
    Acta Biochimica Polonica; 2011, 58, 1; 75-77
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Infrared study of copper(II) complexes with pyridine-3-carboxamide derivatives in chloride media
    Autorzy:
    Borowiak-Resterna, A.
    Olszanowski, A.
    Powiązania:
    https://bibliotekanauki.pl/articles/346901.pdf
    Data publikacji:
    2004
    Wydawca:
    Politechnika Bydgoska im. Jana i Jędrzeja Śniadeckich. Wydział Technologii i Inżynierii Chemicznej
    Tematy:
    infrared spectra
    solvent extraction
    copper(II)
    pyridine-3-carboxamide derivatives
    benzamide derivatives
    Opis:
    The extraction studies for copper(II) from chloride solutions by mono- and dialkyl derivatives of benzamide and pyridine-3-carboxamide show that the coordination of copper by amide groups is very weak, weaker than by chloride ions. N,N-dialkyl derivative of benzamide does not extract copper from chloride media but N-alkylbenzamide eliminates a small amount of copper (a great deal smaller than pyridine-3-carboxamide derivatives) only from diluted chloride aqueous solutions ([Cl-] < 0.1 M). Infrared studies of copper complexes with mono- and dialkylpyridine-3-carboxamides show that coordination of the ligand molecules to copper(II) ions takes place mainly by the pyridine nitrogen. More stable monoalkylpyridinecarboxamides complexes with CuCl2 are formed probably by intermolecular hydrogen bonds between monomeric molecules of CuCl2L2 complex (L – the amide). However, weak coordination of copper(II) by the amide group may take place.
    Źródło:
    Ars Separatoria Acta; 2004, 3; 105-113
    1731-6340
    Pojawia się w:
    Ars Separatoria Acta
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Simple and Efficient Three Component One-pot Synthesis of Pyrazolo[1,5,a]pyrimidines
    Autorzy:
    Morabia, A. R.
    Naliapara, Y. T.
    Powiązania:
    https://bibliotekanauki.pl/articles/411804.pdf
    Data publikacji:
    2015
    Wydawca:
    Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
    Tematy:
    Pyrazolopyrimidine
    5-amino-N-cyclohexyl-3-(methylthio)-1H-pyrazole-4-carboxamide
    1-(2-bromophenyl)-2-nitroethanone
    mild reaction condition
    Opis:
    A series of novel 5-(2-bromophenyl)-N-cyclohexyl-2-(methylthio)-6-nitro-7-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamides were synthesized by a one-pot reaction of 5-amino-N-cyclohexyl-3-(methylthio)-1H-pyrazole-4-carboxamide, 1-(2-bromophenyl)-2-nitroethanone and aryl aldehydes in the presence of boric acid in water at refluxing temperature. Structures of compounds were demonstrated by Fourier transform infrared, 1H NMR, 13C NMR and elemental analysis. The advantages of this method are mild reaction condition, good yields, and operational simplicity.
    Źródło:
    International Letters of Chemistry, Physics and Astronomy; 2015, 41; 73-81
    2299-3843
    Pojawia się w:
    International Letters of Chemistry, Physics and Astronomy
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    SUBSTITUTED CARBOXAMIDE ANALOGUES AS A NEW CLASS OF LOCAL ANESTHETIC AGENTS: SYNTHESIS AND BIO-EVALUATION
    Autorzy:
    AlOtaibi, Faisal
    Powiązania:
    https://bibliotekanauki.pl/articles/895677.pdf
    Data publikacji:
    2018-06-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    hepatotoxicity
    Carboxamide
    surface local anesthetic activity
    infiltration local anesthetic activity
    Opis:
    Abstract: A series of N-(2-oxo-2-(phenylamino) ethyl) substituted-4-carboxamide derivatives were synthesized as local anesthetic agents. The structures of carboxamide derivatives were established on the basis of IR, and 1H spectral data. All the compounds were subjected to surface local anesthetic activity assay and infiltration local anesthetic activity assay. Among the tested compounds, N-(2-oxo-2-(p-tolylamino) ethyl) piperidine-1-carboxamide (4h) and N-(2-((4-methoxyphenyl) amino)-2-oxoethyl) piperidine-1-carboxamide (4m) were most promising compounds in terms of surface local anaesthetic and infiltration local anaesthetic activity on rats having considerably lower liver toxicity. Keywords: Carboxamide, surface local anesthetic activity, infiltration local anesthetic activity, hepatotoxicity.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 3
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis of novel 2-mercapto-4-(p-aminophenyl sulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide derivatives via the Biginelli reaction
    Autorzy:
    Bhuva, N. H.
    Gothalia, V. K.
    Singala, P. M.
    Talpara, P. K.
    Faldu, V. J.
    Shah, V. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/412069.pdf
    Data publikacji:
    2014
    Wydawca:
    Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
    Tematy:
    2-mercapto-4-(p-aminophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide
    Biginelli condensation
    Opis:
    Series of 2-mercapto-4-(p-aminophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide Aa-h were synthesized via the biginelli condensation. 2-mercapto-4-amino-6-(aryl)-pyrimidine-5-carboxamide react with p-acetamidophenylsulphonylchloride in the presence of pyridine 2 to form 2-mercapto-4-(p-acetamidophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide 3. It was treated with diluted HCl under reflux afforded 2-mercapto-4-(p-aminophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide A a-h. The newly synthesized compounds were characterized by elemental analyses, infrared (IR), 1H NMR and 13 C NMR spectroscopic investigation.
    Źródło:
    International Letters of Chemistry, Physics and Astronomy; 2014, 17, 2; 168-173
    2299-3843
    Pojawia się w:
    International Letters of Chemistry, Physics and Astronomy
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Wybrane substancje chłodzące stosowane w kosmetykach
    Selected cooling compounds used in cosmetics
    Autorzy:
    Adaszyńska, M.
    Swarcewicz, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/172597.pdf
    Data publikacji:
    2012
    Wydawca:
    Polskie Towarzystwo Chemiczne
    Tematy:
    substancje chłodzące
    mentol
    pochodne mentolu
    amidy
    kosmetyki
    cooling ingredients
    menthol
    menthol-related
    carboxamide
    cosmetics
    Opis:
    Menthol and new cooling compounds are widely used to improve modern toothpastes, gums, breath fresheners, cosmetic lotions, deodorants, shaving gels, and shaving aid composites. This paper reviews the use of menthol and new classes of cooling agents, that have been discovered since the 1970s, in cosmetic preparations. We have presented here 57 chemical structures. In addition, we briefly touch upon cold receptors and mechanism of action. Finally, we add up, recent findings on the production of cooling ingredients in the world. The underlying process in thermoreception depends on ion transport across cellular membranes. Thermoreceptors belong to a class of transient receptor potential (TRP) channels. Among them are temperature-sensitive thermoreceptors TRPM8 or TRPA 1. Certain types of chemical agonists activate the same thermoTRP channels, as for example menthol or icilin. Only the (–)-menthol enantiomer possesses clean, desirable minty odor and intense cooling properties (Fig. 1). Natural menthol is normally about 99.0% to 99.6% pure, with the remaining impurities being other constituents found in the cornmit oil. Synthetic (–)-menthol is normally about 99.8% pure and has less of the minty top note than the natural menthol. The other natural and synthetic compounds being menthol-related coolants are showed in Figure 3, as for example, menthone 1,2-glycerol ketal (17). From among 3-carboxamide-p-menthane derivatives as commercial cooling agents (Fig. 4), there are for example N-ethyl-pmenthane- 3-carboxamide (25) as WS-3 and [ethyl 3-(p-menthane-3-carboxamido) acetate] as WS-5, which is currently the coldest of all commercial cooling agents (27). Other examples of recently discovered carboxamide coolants belong to a series of analogs of WS-23 (28). Of particular interest are various aryl p-menthane-3- carboxamides, such as N-benzo[1,3]dioxol-5-yl-3-p-menthanecarboxamide (36), which was reported to have 100 times more cooling intensity than menthol (Fig. 6). In 2010, Furrer disclosed a series of new p-menthane carboxamide and WS-23 analogs as cooling agents [56]. Three particularly potential cooling agents 50, 51 and 52 are shown in Figure 9.
    Źródło:
    Wiadomości Chemiczne; 2012, 66, 5-6; 543-562
    0043-5104
    2300-0295
    Pojawia się w:
    Wiadomości Chemiczne
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-7 z 7

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