Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities

Detalhes bibliográficos
Autor(a) principal: MONTE,ZENAIDE S.
Data de Publicação: 2017
Outros Autores: SILVA,AMANDA M., LIMA,GLÁUCIA M.S., SILVA,TERESINHA G. DA, MARQUES,KARLA M.R., RODRIGUES,MARIA D., FALCÃO,EMERSON P.S., MELO,SEBASTIÃO J.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Anais da Academia Brasileira de Ciências (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652017000301051
Resumo: ABSTRACT A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity.
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spelling Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activitiesarylamidines2D spectroscopygram-negative bacteriayeastcytotoxicityABSTRACT A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity.Academia Brasileira de Ciências2017-06-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652017000301051Anais da Academia Brasileira de Ciências v.89 n.2 2017reponame:Anais da Academia Brasileira de Ciências (Online)instname:Academia Brasileira de Ciências (ABC)instacron:ABC10.1590/0001-3765201720160801info:eu-repo/semantics/openAccessMONTE,ZENAIDE S.SILVA,AMANDA M.LIMA,GLÁUCIA M.S.SILVA,TERESINHA G. DAMARQUES,KARLA M.R.RODRIGUES,MARIA D.FALCÃO,EMERSON P.S.MELO,SEBASTIÃO J.eng2017-06-07T00:00:00Zoai:scielo:S0001-37652017000301051Revistahttp://www.scielo.br/aabchttps://old.scielo.br/oai/scielo-oai.php||aabc@abc.org.br1678-26900001-3765opendoar:2017-06-07T00:00Anais da Academia Brasileira de Ciências (Online) - Academia Brasileira de Ciências (ABC)false
dc.title.none.fl_str_mv Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
title Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
spellingShingle Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
MONTE,ZENAIDE S.
arylamidines
2D spectroscopy
gram-negative bacteria
yeast
cytotoxicity
title_short Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
title_full Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
title_fullStr Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
title_full_unstemmed Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
title_sort Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
author MONTE,ZENAIDE S.
author_facet MONTE,ZENAIDE S.
SILVA,AMANDA M.
LIMA,GLÁUCIA M.S.
SILVA,TERESINHA G. DA
MARQUES,KARLA M.R.
RODRIGUES,MARIA D.
FALCÃO,EMERSON P.S.
MELO,SEBASTIÃO J.
author_role author
author2 SILVA,AMANDA M.
LIMA,GLÁUCIA M.S.
SILVA,TERESINHA G. DA
MARQUES,KARLA M.R.
RODRIGUES,MARIA D.
FALCÃO,EMERSON P.S.
MELO,SEBASTIÃO J.
author2_role author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv MONTE,ZENAIDE S.
SILVA,AMANDA M.
LIMA,GLÁUCIA M.S.
SILVA,TERESINHA G. DA
MARQUES,KARLA M.R.
RODRIGUES,MARIA D.
FALCÃO,EMERSON P.S.
MELO,SEBASTIÃO J.
dc.subject.por.fl_str_mv arylamidines
2D spectroscopy
gram-negative bacteria
yeast
cytotoxicity
topic arylamidines
2D spectroscopy
gram-negative bacteria
yeast
cytotoxicity
description ABSTRACT A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity.
publishDate 2017
dc.date.none.fl_str_mv 2017-06-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652017000301051
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652017000301051
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/0001-3765201720160801
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv Academia Brasileira de Ciências
publisher.none.fl_str_mv Academia Brasileira de Ciências
dc.source.none.fl_str_mv Anais da Academia Brasileira de Ciências v.89 n.2 2017
reponame:Anais da Academia Brasileira de Ciências (Online)
instname:Academia Brasileira de Ciências (ABC)
instacron:ABC
instname_str Academia Brasileira de Ciências (ABC)
instacron_str ABC
institution ABC
reponame_str Anais da Academia Brasileira de Ciências (Online)
collection Anais da Academia Brasileira de Ciências (Online)
repository.name.fl_str_mv Anais da Academia Brasileira de Ciências (Online) - Academia Brasileira de Ciências (ABC)
repository.mail.fl_str_mv ||aabc@abc.org.br
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