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dc.contributor.author
Pagliero, Romina Julieta
dc.contributor.author
Pierini, Adriana Beatriz
dc.contributor.author
Brun, R.
dc.contributor.author
Mazzieri, Maria Rosa
dc.date.available
2019-02-11T14:38:26Z
dc.date.issued
2010-10
dc.identifier.citation
Pagliero, Romina Julieta; Pierini, Adriana Beatriz; Brun, R.; Mazzieri, Maria Rosa; Design, synthesis and 3-d characterization of 1-benzenesulfonyl-1,2,3,4-tetrahydroquinolines as lead scaffold for antiparasitic drug; Bentham Science Publishers; Letters In Drug Design & Discovery; 7; 6; 10-2010; 461-470
dc.identifier.issn
1570-1808
dc.identifier.uri
http://hdl.handle.net/11336/69834
dc.description.abstract
Ten 1-benzenesulfonyl-1,2,3,4-tetrahydroquinoline (BSTHQ) were synthesized and characterized and their antiprotozoal activities were investigated. This small library was designed by combining two chemical moieties that are known to be biologically active by itself. The BS group seems to be favorable for the antiparasitic activity, since the derivatives presented lower IC50 value than the precursor heterocycle. Most compounds were moderately active against T cruzi, but 3 showed a promising IC50 value (9.76μM) with low cytotoxicity (L6). Also, 3, 6 and 9 showed interesting activity and reasonable selectivity against P. falciparum. These derivatives are considered as lead scaffolds and merit further exploration through structure optimization.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Bentham Science Publishers
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Antiparasitic
dc.subject
Benzenesulfonyl
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Tetrahydroquinolines
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Stereoelectronic Properties
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Otras Ciencias Químicas
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Design, synthesis and 3-d characterization of 1-benzenesulfonyl-1,2,3,4-tetrahydroquinolines as lead scaffold for antiparasitic drug
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2019-01-14T15:02:13Z
dc.identifier.eissn
1875-628X
dc.journal.volume
7
dc.journal.number
6
dc.journal.pagination
461-470
dc.journal.pais
Estados Unidos
dc.journal.ciudad
Oak Park
dc.description.fil
Fil: Pagliero, Romina Julieta. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones en Físico-química de Córdoba. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Instituto de Investigaciones en Físico-química de Córdoba; Argentina
dc.description.fil
Fil: Pierini, Adriana Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones en Físico-química de Córdoba. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Instituto de Investigaciones en Físico-química de Córdoba; Argentina
dc.description.fil
Fil: Brun, R.. Parasite Chemotherapy, Swiss Tropical Institute; Suiza
dc.description.fil
Fil: Mazzieri, Maria Rosa. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina
dc.journal.title
Letters In Drug Design & Discovery
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.ingentaconnect.com/content/ben/lddd/2010/00000007/00000006/012aj
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://doi.org/10.2174/157018010791306614
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