New Potentially Active Pyrazinamide Derivatives Synthesized Under Microwave Conditions

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F14%3A10282204" target="_blank" >RIV/00216208:11160/14:10282204 - isvavai.cz</a>

Result on the web

<a href="http://www.mdpi.com/1420-3049/19/7/9318/htm" target="_blank" >http://www.mdpi.com/1420-3049/19/7/9318/htm</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules19079318" target="_blank" >10.3390/molecules19079318</a>

Result language

angličtina

Original language name

New Potentially Active Pyrazinamide Derivatives Synthesized Under Microwave Conditions

Original language description

A series of 18 N-alkyl substituted 3-aminopyrazine-2-carboxamides was prepared in this work according to previously experimentally set and proven conditions using microwave assisted synthesis methodology. This approach for the aminodehalogenation reaction was chosen due to higher yields and shorter reaction times compared to organic reactions with conventional heating. Antimycobacterial, antibacterial, antifungal and photosynthetic electron transport (PET) inhibiting in vitro activities of these compounds were investigated. Experiments for the determination of lipophilicity were also performed. Only a small number of substances with alicyclic side chain showed activity against fungi which was the same or higher than standards and the biological efficacy of the compounds increased with rising lipophilicity. Nine pyrazinamide derivatives also inhibited PET in spinach chloroplasts and the IC50 values of these compounds varied in the range from 14.3 to 1590.0 mu mol/L. The inhibitory activ

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

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

Publication year

2014

Confidentiality

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

Name of the periodical

Molecules

ISSN

1420-3049

e-ISSN

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Volume of the periodical

19

Issue of the periodical within the volume

7

Country of publishing house

CH - SWITZERLAND

Number of pages

21

Pages from-to

9318-9338

UT code for WoS article

000340036200039

EID of the result in the Scopus database

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