Synthesis and Antimicrobial Evaluation of 6-Alkylamino-N-phenylpyrazine-2-carboxamides

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F15%3A10312185" target="_blank" >RIV/00216208:11160/15:10312185 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00179906:_____/15:10312185

Výsledek na webu

<a href="http://onlinelibrary.wiley.com/doi/10.1111/cbdd.12536/full" target="_blank" >http://onlinelibrary.wiley.com/doi/10.1111/cbdd.12536/full</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1111/cbdd.12536" target="_blank" >10.1111/cbdd.12536</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Synthesis and Antimicrobial Evaluation of 6-Alkylamino-N-phenylpyrazine-2-carboxamides

Popis výsledku v původním jazyce

This work presents synthesis and antimicrobial evaluation of nineteen 6-alkylamino-N-phenylpyrazine-2-carboxamides. Antimycobacterial activity was determined against Mycobacterium tuberculosis H37Rv, M.kansasii and two strains of M.avium. Generally, theantimycobacterial activity increased with prolongation of simple alkyl chain and culminated in compounds with heptylamino substitution (3e, 4e) with MIC=5-10m against M.tuberculosis H37Rv. On the contrary, derivatives with modified alkyl chain (containing e.g. terminal methoxy or hydroxy group) as well as phenylalkylamino derivatives were mainly inactive. The most active compounds (with hexyl to octylamino substitution) were evaluated for their in vitro activity against drug-resistant strains of M.tuberculosis and possessed activity comparable to that of the reference drug isoniazid. None of the tested compounds were active against M.avium. Some derivatives exhibited activity against Gram-positive bacteria including methicillin-resistan

Název v anglickém jazyce

Synthesis and Antimicrobial Evaluation of 6-Alkylamino-N-phenylpyrazine-2-carboxamides

Popis výsledku anglicky

This work presents synthesis and antimicrobial evaluation of nineteen 6-alkylamino-N-phenylpyrazine-2-carboxamides. Antimycobacterial activity was determined against Mycobacterium tuberculosis H37Rv, M.kansasii and two strains of M.avium. Generally, theantimycobacterial activity increased with prolongation of simple alkyl chain and culminated in compounds with heptylamino substitution (3e, 4e) with MIC=5-10m against M.tuberculosis H37Rv. On the contrary, derivatives with modified alkyl chain (containing e.g. terminal methoxy or hydroxy group) as well as phenylalkylamino derivatives were mainly inactive. The most active compounds (with hexyl to octylamino substitution) were evaluated for their in vitro activity against drug-resistant strains of M.tuberculosis and possessed activity comparable to that of the reference drug isoniazid. None of the tested compounds were active against M.avium. Some derivatives exhibited activity against Gram-positive bacteria including methicillin-resistan

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Chemical Biology and Drug Design

ISSN

1747-0277

e-ISSN

—

Svazek periodika

86

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

DK - Dánské království

Počet stran výsledku

8

Strana od-do

674-681

Kód UT WoS článku

000362163500031

EID výsledku v databázi Scopus

2-s2.0-84942503217