Activity of ring-substituted 8-hydroxyquinoline-2-carboxanilides against intestinal sulfate-reducing bacteria Desulfovibrio piger

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F18%3A43876764" target="_blank" >RIV/62157124:16370/18:43876764 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216224:14310/18:00102042

Výsledek na webu

<a href="https://www.researchgate.net/publication/323108334_Effect_of_selected_8-hydroxyquinoline-2-carboxanilides_on_viability_and_sulfate_metabolism_of_Desulfovibrio_piger" target="_blank" >https://www.researchgate.net/publication/323108334_Effect_of_selected_8-hydroxyquinoline-2-carboxanilides_on_viability_and_sulfate_metabolism_of_Desulfovibrio_piger</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1007/s00044-017-2067-7" target="_blank" >10.1007/s00044-017-2067-7</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Activity of ring-substituted 8-hydroxyquinoline-2-carboxanilides against intestinal sulfate-reducing bacteria Desulfovibrio piger

Popis výsledku v původním jazyce

Desulfovibrio genus is dominant among sulfate-reducing bacteria (SRB) in the large intestine of healthy people and animals. It is mostly isolated from patients with inflammatory bowel disease (IBD) and can be involved in the disease initiation. Primary in vitro screening of 8-hydroxyquinoline-2-carboxanilides was performed against Desulfovibrio piger Vib-7 representing SRB. The most effective compounds with MIC90/MBC values in the range of 17-23 mu M/20-23 mu M, respectively, were substituted in C&apos;((3)) by CF3, OCH3, CH3 and in C&apos;((4)) by CF3. Their activity was twofold higher than that of ciprofloxacin. These compounds did not express any significant cytotoxic effect on THP-1 cells up to the tested concentration of 30 mu M. The antibacterial efficacy of the most active C&apos;((3))-substituted compounds practically did not change with increasing compound lipophilicity, indicating that this position of substitution is favorable for significant antimicrobial effect, while the antibacterial activity of most of C&apos;((2)) and C&apos;((4))-substituted derivatives decreased linearly with increasing compound lipophilicity. In addition, the dependence of activity on electronic Hammett&apos;s sigma parameter of the substituent R was quasi-parabolic for the most effective C&apos;((3))-substituted compounds.

Název v anglickém jazyce

Activity of ring-substituted 8-hydroxyquinoline-2-carboxanilides against intestinal sulfate-reducing bacteria Desulfovibrio piger

Popis výsledku anglicky

Desulfovibrio genus is dominant among sulfate-reducing bacteria (SRB) in the large intestine of healthy people and animals. It is mostly isolated from patients with inflammatory bowel disease (IBD) and can be involved in the disease initiation. Primary in vitro screening of 8-hydroxyquinoline-2-carboxanilides was performed against Desulfovibrio piger Vib-7 representing SRB. The most effective compounds with MIC90/MBC values in the range of 17-23 mu M/20-23 mu M, respectively, were substituted in C&apos;((3)) by CF3, OCH3, CH3 and in C&apos;((4)) by CF3. Their activity was twofold higher than that of ciprofloxacin. These compounds did not express any significant cytotoxic effect on THP-1 cells up to the tested concentration of 30 mu M. The antibacterial efficacy of the most active C&apos;((3))-substituted compounds practically did not change with increasing compound lipophilicity, indicating that this position of substitution is favorable for significant antimicrobial effect, while the antibacterial activity of most of C&apos;((2)) and C&apos;((4))-substituted derivatives decreased linearly with increasing compound lipophilicity. In addition, the dependence of activity on electronic Hammett&apos;s sigma parameter of the substituent R was quasi-parabolic for the most effective C&apos;((3))-substituted compounds.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10606 - Microbiology

Projekt

—

Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2018

Kód důvěrnosti údajů

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

Název periodika

Medicinal chemistry research

ISSN

1054-2523

e-ISSN

—

Svazek periodika

27

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

7

Strana od-do

278-284

Kód UT WoS článku

000419972400025

EID výsledku v databázi Scopus

—