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Statements

Subject Item
n2:RIV%2F62157124%3A16370%2F07%3A00001121%21RIV08-MSM-16370___
rdf:type
n7:Vysledek skos:Concept
dcterms: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). 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. 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).
dcterms:title
Substituované pyrazin-2,5-dikarboxamidy: syntéza, hydrofobní parametry a antimykobakteriální hodnocení Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation
skos:prefLabel
Substituované pyrazin-2,5-dikarboxamidy: syntéza, hydrofobní parametry a antimykobakteriální hodnocení Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation
skos:notation
RIV/62157124:16370/07:00001121!RIV08-MSM-16370___
n3:strany
005-015
n3:aktivita
n19:S
n3:aktivity
S
n3:dodaniDat
n8:2008
n3:domaciTvurceVysledku
n16:9033793
n3:druhVysledku
n10:D
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n18:predkladatel
n3:idSjednocenehoVysledku
453429
n3:idVysledku
RIV/62157124:16370/07:00001121
n3:jazykVysledku
n5:eng
n3:klicovaSlova
Pyrazinecarboxamides; In vitro antimycobacterial activity; Lipophilicity determination
n3:klicoveSlovo
n15:Pyrazinecarboxamides n15:In%20vitro%20antimycobacterial%20activity n15:Lipophilicity%20determination
n3:kontrolniKodProRIV
[DD52AB81C381]
n3:mistoVydani
Basel
n3:nazevZdroje
Proceedings of 11th International Electronic Conference on Synthetic Organic Chemistry
n3:obor
n13:FR
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
4
n3:rokUplatneniVysledku
n8:2007
n3:tvurceVysledku
Doležal, Martin Bielesz, Stanislav Kuneš, Jiří Jampílek, Josef
s:numberOfPages
11
n9:hasPublisher
Molecular Diversity Preservation International (MDPI)
n14:isbn
3-906980-19-7
n11:organizacniJednotka
16370