Substituované pyrazin-2,5-dikarboxamidy: syntéza, hydrofobní parametry a antimykobakteriální hodnocení

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F07%3A00001121" target="_blank" >RIV/62157124:16370/07:00001121 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation

Popis výsledku v původním jazyce

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 commerciallyavailable 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 ofthe evaluated compounds are discussed. 3-(3-Methylphenyl)-aminopyrazine-2,5- dicarboxamide (7) has shown the highest activity against M. tuberculosis H37Rv (63% inhibition).

Název v anglickém jazyce

Substituted pyrazine-2,5-dicarboxamides: Synthesis, Hydrophobicity Parameters and Antimycobacterial Evaluation

Popis výsledku anglicky

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 commerciallyavailable 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 ofthe evaluated compounds are discussed. 3-(3-Methylphenyl)-aminopyrazine-2,5- dicarboxamide (7) has shown the highest activity against M. tuberculosis H37Rv (63% inhibition).

Druh

D - Stať ve sborníku

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2007

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název statě ve sborníku

Proceedings of 11th International Electronic Conference on Synthetic Organic Chemistry

ISBN

3-906980-19-7

ISSN

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e-ISSN

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Počet stran výsledku

11

Strana od-do

005-015

Název nakladatele

Molecular Diversity Preservation International (MDPI)

Místo vydání

Basel

Místo konání akce

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Datum konání akce

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Typ akce podle státní příslušnosti

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Kód UT WoS článku

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