Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols

Detalhes bibliográficos
Autor(a) principal: Kerr,David I. B.
Data de Publicação: 2007
Outros Autores: Khalafy,Jabbar, Ong,Jennifer, Prager,Rolf H., Rimaz,Mehdi
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Journal of the Brazilian Chemical Society (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532007000400009
Resumo: A series of six 2,2-disubstituted 3-[3,5-di-iso-propyl-4-hydroxyphenyl]propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABA B receptors. The activity (EC50 30 µM) was greatest for the dimethyl analogue, but the isopropylphenyl compounds were generally weaker than the corresponding t-butyl compounds. Methylation of the phenolic group led to loss of activity.
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spelling Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanolspropofol analogueallosteric positive modulationGABA BA series of six 2,2-disubstituted 3-[3,5-di-iso-propyl-4-hydroxyphenyl]propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABA B receptors. The activity (EC50 30 µM) was greatest for the dimethyl analogue, but the isopropylphenyl compounds were generally weaker than the corresponding t-butyl compounds. Methylation of the phenolic group led to loss of activity.Sociedade Brasileira de Química2007-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532007000400009Journal of the Brazilian Chemical Society v.18 n.4 2007reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0103-50532007000400009info:eu-repo/semantics/openAccessKerr,David I. B.Khalafy,JabbarOng,JenniferPrager,Rolf H.Rimaz,Mehdieng2007-09-18T00:00:00Zoai:scielo:S0103-50532007000400009Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2007-09-18T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false
dc.title.none.fl_str_mv Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
title Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
spellingShingle Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
Kerr,David I. B.
propofol analogue
allosteric positive modulation
GABA B
title_short Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
title_full Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
title_fullStr Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
title_full_unstemmed Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
title_sort Synthesis and biological activity of allosteric modulators of GABA B receptors part 3. 3-(2,6-bis-iso-propyl-4-hydroxyphenyl)propanols
author Kerr,David I. B.
author_facet Kerr,David I. B.
Khalafy,Jabbar
Ong,Jennifer
Prager,Rolf H.
Rimaz,Mehdi
author_role author
author2 Khalafy,Jabbar
Ong,Jennifer
Prager,Rolf H.
Rimaz,Mehdi
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Kerr,David I. B.
Khalafy,Jabbar
Ong,Jennifer
Prager,Rolf H.
Rimaz,Mehdi
dc.subject.por.fl_str_mv propofol analogue
allosteric positive modulation
GABA B
topic propofol analogue
allosteric positive modulation
GABA B
description A series of six 2,2-disubstituted 3-[3,5-di-iso-propyl-4-hydroxyphenyl]propan-1-ol derivatives have been prepared for evaluation as allosteric modulators of GABA B receptors. The activity (EC50 30 µM) was greatest for the dimethyl analogue, but the isopropylphenyl compounds were generally weaker than the corresponding t-butyl compounds. Methylation of the phenolic group led to loss of activity.
publishDate 2007
dc.date.none.fl_str_mv 2007-01-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532007000400009
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532007000400009
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S0103-50532007000400009
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 Sociedade Brasileira de Química
publisher.none.fl_str_mv Sociedade Brasileira de Química
dc.source.none.fl_str_mv Journal of the Brazilian Chemical Society v.18 n.4 2007
reponame:Journal of the Brazilian Chemical Society (Online)
instname:Sociedade Brasileira de Química (SBQ)
instacron:SBQ
instname_str Sociedade Brasileira de Química (SBQ)
instacron_str SBQ
institution SBQ
reponame_str Journal of the Brazilian Chemical Society (Online)
collection Journal of the Brazilian Chemical Society (Online)
repository.name.fl_str_mv Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)
repository.mail.fl_str_mv ||office@jbcs.sbq.org.br
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