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| Description
| - Substituted pyrazine derivatives were synthesized and tested against Mycobacterium tuberculosis strain H37Rv. The hydrophobicity of all the pyrazines was determined using the reversed phase high performance liquid chromatography (RP-HPLC) method (isocratic elution with methanol as an organic modifier in the mobile phase, end-capped non-polar C18 stationary RP column). Experimentally derived Log K values (the logarithm of capacity factor K) were that compared with Log P values calculated by commercially available programmes. The synthetic approach, analytical, spectroscopic, lipophilicity and biological data of ten newly synthesized compounds are presented. Structure?activity relationships among the chemical structure, the antimycobacterial activity of the evaluated compounds are discussed. 3-(3-Methylphenyl)-aminopyrazine-2,5- dicarboxamide (7) has shown the highest activity against M. tuberculosis H37Rv (63% inhibition).
- Substituted pyrazine derivatives were synthesized and tested against Mycobacterium tuberculosis strain H37Rv. The hydrophobicity of all the pyrazines was determined using the reversed phase high performance liquid chromatography (RP-HPLC) method (isocratic elution with methanol as an organic modifier in the mobile phase, end-capped non-polar C18 stationary RP column). Experimentally derived Log K values (the logarithm of capacity factor K) were that compared with Log P values calculated by commercially available programmes. The synthetic approach, analytical, spectroscopic, lipophilicity and biological data of ten newly synthesized compounds are presented. Structure?activity relationships among the chemical structure, the antimycobacterial activity of the evaluated compounds are discussed. 3-(3-Methylphenyl)-aminopyrazine-2,5- dicarboxamide (7) has shown the highest activity against M. tuberculosis H37Rv (63% inhibition). (en)
- Substituované deriváty pyrazinu byly připraveny a testovány proti Mycobacterium tuberculosis, kmen H37Rv. Hydrofobicita všech pyrazinových derivátů by stanovena pomocí metody RP-HPLC (isokratická eluce mobilní fází s methanolem jako organickým modifikátorem, kolona s C18 endkapovanou nepolární stacionární fází). Experimentálně zjištěné hodnoty log K byly porovnány s hodnotami log P vypočítanými komerčně dostupnými programy. V článku je prezentována syntéza, analytická, lipofilitní a biologická data deseti nově syntetizovaných látek. Vztahy mezi strukturou a antimykobakteriální aktivitou jsou obsaženy v diskusi. Nejvyšší aktivitu proti M. tuberculosis H37Rv vykázal 3-(3-Methylfenyl)-aminopyrazin-2,5-dicarboxamid (7) ? 63% inhibice. (cs)
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| Title
| - Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation
- Substituované pyrazin-2,5-dikarboxamidy: syntéza, hydrofobní parametry a antimykobakteriální hodnocení (cs)
- Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation (en)
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| skos:prefLabel
| - Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation
- Substituované pyrazin-2,5-dikarboxamidy: syntéza, hydrofobní parametry a antimykobakteriální hodnocení (cs)
- Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation (en)
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| skos:notation
| - RIV/62157124:16370/07:00001121!RIV08-MSM-16370___
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| http://linked.open.../vavai/riv/strany
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/62157124:16370/07:00001121
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - Pyrazinecarboxamides; In vitro antimycobacterial activity; Lipophilicity determination (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/mistoVydani
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| http://linked.open...i/riv/nazevZdroje
| - Proceedings of 11th International Electronic Conference on Synthetic Organic Chemistry
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
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| http://linked.open...UplatneniVysledku
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| http://linked.open...iv/tvurceVysledku
| - Doležal, Martin
- Jampílek, Josef
- Kuneš, Jiří
- Bielesz, Stanislav
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| number of pages
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| http://purl.org/ne...btex#hasPublisher
| - Molecular Diversity Preservation International (MDPI)
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| https://schema.org/isbn
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| http://localhost/t...ganizacniJednotka
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| is http://linked.open...avai/riv/vysledek
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