SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY

Claisen condensation of ethyl isonicotinate with different acetophenones gave the corresponding pyridyl-ß-diketones, while the treatment with hydrazine hydrate yielded 3,5-disubstituted-1H-pyrazoles, which then converted 1,3,5-trisubstituted-pyrazole derivatives containing a pyridyl moiety by N-acyl...

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Autores principales: WANG,DUN-JIA, LIU,HUA, KANG,YAN-FANG, HU,YAN-JUN, WEI,XIAN-HONG
Lenguaje:English
Publicado: Sociedad Chilena de Química 2015
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Acceso en línea:http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072015000100018
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spelling oai:scielo:S0717-970720150001000182015-04-21SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETYWANG,DUN-JIALIU,HUAKANG,YAN-FANGHU,YAN-JUNWEI,XIAN-HONG 1,3,5-Trisubstituted-pyrazole ß-Diketone Synthesis, Anti-microbial activity Claisen condensation of ethyl isonicotinate with different acetophenones gave the corresponding pyridyl-ß-diketones, while the treatment with hydrazine hydrate yielded 3,5-disubstituted-1H-pyrazoles, which then converted 1,3,5-trisubstituted-pyrazole derivatives containing a pyridyl moiety by N-acylation with acyl chloride. The structures of all newly synthesized compounds are established by FTIR, ¹H NMR, mass spectroscopy and elemental analysis, and in the case of compound 2e, analyzed by single-crystal X-ray diffraction further. The anti-microbial activities of the title compounds have been tested by disc diffusion method against Escherichia coli, Staphylococcus aureus, Pyricularia oryzae and Rhizoctnia solani. The results showed that compounds 3c and 4c exhibited good inhibitory activity against all the tested organisms.info:eu-repo/semantics/openAccessSociedad Chilena de QuímicaJournal of the Chilean Chemical Society v.60 n.1 20152015-03-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072015000100018en10.4067/S0717-97072015000100018
institution Scielo Chile
collection Scielo Chile
language English
topic 1,3,5-Trisubstituted-pyrazole
ß-Diketone
Synthesis, Anti-microbial activity
spellingShingle 1,3,5-Trisubstituted-pyrazole
ß-Diketone
Synthesis, Anti-microbial activity
WANG,DUN-JIA
LIU,HUA
KANG,YAN-FANG
HU,YAN-JUN
WEI,XIAN-HONG
SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY
description Claisen condensation of ethyl isonicotinate with different acetophenones gave the corresponding pyridyl-ß-diketones, while the treatment with hydrazine hydrate yielded 3,5-disubstituted-1H-pyrazoles, which then converted 1,3,5-trisubstituted-pyrazole derivatives containing a pyridyl moiety by N-acylation with acyl chloride. The structures of all newly synthesized compounds are established by FTIR, ¹H NMR, mass spectroscopy and elemental analysis, and in the case of compound 2e, analyzed by single-crystal X-ray diffraction further. The anti-microbial activities of the title compounds have been tested by disc diffusion method against Escherichia coli, Staphylococcus aureus, Pyricularia oryzae and Rhizoctnia solani. The results showed that compounds 3c and 4c exhibited good inhibitory activity against all the tested organisms.
author WANG,DUN-JIA
LIU,HUA
KANG,YAN-FANG
HU,YAN-JUN
WEI,XIAN-HONG
author_facet WANG,DUN-JIA
LIU,HUA
KANG,YAN-FANG
HU,YAN-JUN
WEI,XIAN-HONG
author_sort WANG,DUN-JIA
title SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY
title_short SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY
title_full SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY
title_fullStr SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY
title_full_unstemmed SYNTHESIS AND ANTI-MICROBIAL ACTIVITIES OF 1,3,5-TRISUBSTITUTED-PYRAZOLE DERIVATIVES CONTAINING A PYRIDYL MOIETY
title_sort synthesis and anti-microbial activities of 1,3,5-trisubstituted-pyrazole derivatives containing a pyridyl moiety
publisher Sociedad Chilena de Química
publishDate 2015
url http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072015000100018
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