About: Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	A series of 14 new compounds related to pyrazinamide were synthesized, characterized with analytical data and screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and two types of Mycobacterium avium. The series comprised of N-substituted 3-aminopyrazine- 2,5-dicarbonitriles derived from 3-chloropyrazine-2,5-dicarbonitrile by nucleophilic substitution of chlorine by various non-aromatic amines (alkylamines, cycloalkylamines and heterocyclic amines). Noteworthy antimycobacterial activity against M. tuberculosis was found among the alkylamino derivatives, for example, 3-(heptylamino) pyrazine-2,5-dicarbonitrile inhibited M. tuberculosis at MIC = 51 mu mol/L. 3-(Hexylamino) pyrazine-2,5-dicarbonitrile inhibited M. kansasii at MIC = 218 mu mol/L. Basic structure-activity relationships are discussed. A comparison between calculated and experimentally determined lipophilicity parameters within the series is included. A series of 14 new compounds related to pyrazinamide were synthesized, characterized with analytical data and screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and two types of Mycobacterium avium. The series comprised of N-substituted 3-aminopyrazine- 2,5-dicarbonitriles derived from 3-chloropyrazine-2,5-dicarbonitrile by nucleophilic substitution of chlorine by various non-aromatic amines (alkylamines, cycloalkylamines and heterocyclic amines). Noteworthy antimycobacterial activity against M. tuberculosis was found among the alkylamino derivatives, for example, 3-(heptylamino) pyrazine-2,5-dicarbonitrile inhibited M. tuberculosis at MIC = 51 mu mol/L. 3-(Hexylamino) pyrazine-2,5-dicarbonitrile inhibited M. kansasii at MIC = 218 mu mol/L. Basic structure-activity relationships are discussed. A comparison between calculated and experimentally determined lipophilicity parameters within the series is included. (en)
Title	Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles (en)
skos:prefLabel	Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles (en)
skos:notation	RIV/62157124:16370/12:43871112!RIV13-MSM-16370___
http://linked.open...avai/predkladatel	Farmaceutická fakulta
http://linked.open...avai/riv/aktivita	I P S V Z
http://linked.open...avai/riv/aktivity	I, P(NS10367), S, V, Z(MSM0021620822)
http://linked.open...iv/cisloPeriodika	4
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Jampílek, Josef
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Veterinární a farmaceutická univerzita Brno / Farmaceutická fakulta
http://linked.open...dnocenehoVysledku	172910
http://linked.open...ai/riv/idVysledku	RIV/62157124:16370/12:43871112
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Structure-activity relationships; Pyrazinamide derivatives; Lipophilicity; Antimycobacterial activity; Alkyl chain homology (en)
http://linked.open.../riv/klicoveSlovo	Antimycobacterial activity Lipophilicity Structure-activity relationships Alkyl chain homology Pyrazinamide derivatives
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[7F7A00F06E29]
http://linked.open...i/riv/nazevZdroje	Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	Evaluation and development of new perspective antimycobacterial drugs and prodrugs active against multidrug resistant strains
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	22
http://linked.open...iv/tvurceVysledku	Doležal, Martin Jampílek, Josef Kuneš, Jiří Zitko, Jan Svobodová, Michaela Dobrovolný, Lukáš
http://linked.open...ain/vavai/riv/wos	000300404900022
http://linked.open...n/vavai/riv/zamer	Research of new drug structures
issn	0960-894X
number of pages	4 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmcl.2011.12.129
http://localhost/t...ganizacniJednotka	16370
is http://linked.open...avai/riv/vysledek of	Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles

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