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    Wyświetlanie 1-9 z 9
    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:
    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:
    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:
    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:
    Inhibition of RNA synthesis in vitro by 9-aminoacridine carboxamide antitumor agents. Effects on overall RNA synthesis and synthesis of the initiating dinucleotide
    Autorzy:
    Piestrzeniewicz, Mariola
    Czyż, Małgorzata
    Denny, William
    Gniazdowski, Marek
    Powiązania:
    https://bibliotekanauki.pl/articles/1045776.pdf
    Data publikacji:
    1990
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Źródło:
    Acta Biochimica Polonica; 1990, 37, 2; 299-307
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and characterization of diversely substituted pyrimidine-3-carboxamide and their antimicrobial evaluation
    Autorzy:
    Senjani, Hardik K.
    Joshi, H. D.
    Powiązania:
    https://bibliotekanauki.pl/articles/1031771.pdf
    Data publikacji:
    2020
    Wydawca:
    Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
    Tematy:
    1-4-dihydropyrimidine
    analgesic
    anti-inflammatory
    antibacterial
    anticonvulsant
    antifungal
    antimicrobial
    antituberculosis
    antitumor
    biginalli
    dihydropyrimidine
    insecticidal
    multi-component reaction
    pyrimidine
    Opis:
    Pyrimidine related fused heterocycles are attracted to every chemist during the last decade for their biological and chemotherapeutic importance. Pyrimidine derivatives play a vital role in their broad spectrum of biological activities including antituberculosis, anticonvulsant, anti-inflammatory, insecticidal, antifungal, analgesic, and antitumor properties and there of interest as potential bioactive molecules. The nitrogen-containing fragment may be an amidine, urea, thiourea, or guanidine, and adamantine homologs and aromatic aldehyde serve as an excellent illustrative example in that it readily undergoes as Biginali MCRs reaction. Pyrimidines and their derivatives are considered to be important for drugs and agricultural chemicals. Pyrimidine derivatives possess several interesting biological activities. Pyrimidine is a basic nucleus in DNA & RNA, it is associated with diverse biological activities so, we have designed and prepared a novel highly functionalized pyrimidine library of 1,4 DHP and DHPM via a one-pot multi-component (MCRs) synthesis and we screened for antimicrobial activity against various strains.
    Źródło:
    World Scientific News; 2020, 150; 39-77
    2392-2192
    Pojawia się w:
    World Scientific News
    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:
    Inhibition of the helicase activity of HCV NTPase/helicase by 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxamide-5-triphosphate (ribavirin-TP).
    Autorzy:
    Borowski, Peter
    Lang, Melanie
    Niebuhr, Andreas
    Haag, Annemarie
    Schmitz, Herbert
    Schulze zur Wiesch, Julian
    Choe, Joonho
    Siwecka, Maria
    Kulikowski, Tadeusz
    Powiązania:
    https://bibliotekanauki.pl/articles/1044103.pdf
    Data publikacji:
    2001
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    ribavirin-5'-triphosphate
    enzyme inhibition
    HCV helicase
    Opis:
    In the presented study the ribavirin-TP - an established inhibitor of the NTPase activity of the superfamily NTPase/helicases II - was investigated as an inhibitor of the unwinding activity of the hepatitis C virus (HCV) NTPase/helicase. The kinetics of the reaction revealed that ribavirin-TP reduces the turnover number of the helicase reaction by a mechanism that does not correspond to that of the inhibition of the NTPase activity. Our results suggest that derivatives of ribavirin-TP with enhanced stability towards hydrolytic attack may be effective inhibitors of the enzyme.
    Źródło:
    Acta Biochimica Polonica; 2001, 48, 3; 739-744
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-9 z 9

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