Design, synthesis and antimalarial evaluation of novel thiazole derivatives
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Scholar |
Otros documentos de la autoría: Bueno, José María; Carda, Miguel; Crespo, Benigno; Cuñat, Ana Carmen; De Cozar, Cristina; León, María Luisa; Marco, J. Alberto; Roda, Nuria; Sanz-Cervera, Juan F.
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http://dx.doi.org/10.1016/j.bmcl.2016.07.010 |
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Título
Design, synthesis and antimalarial evaluation of novel thiazole derivativesAutoría
Fecha de publicación
2016Editor
ElsevierISSN
0960-894XCita bibliográfica
BUENO, José María, et al. Design, synthesis and antimalarial evaluation of novel thiazole derivatives. Bioorganic & Medicinal Chemistry Letters, 2016, vol. 26, no 16, p. 3938-3944.Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
http://bs8lz6ys5q.search.serialssolutions.com/?ctx_ver=Z39.88-2004&ctx_enc=info% ...Palabras clave / Materias
Resumen
As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the ... [+]
As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain. The results indicate that modifications of the N-aryl amide group linked to the thiazole ring are the most significant in terms of in vitro antimalarial activity, leading to compounds with high antimalarial potency and low cytotoxicity in HepG2 cell lines. Furthermore, the observed SAR implies that non-bulky, electron-withdrawing groups are preferred at ortho position on the phenyl ring, whereas small atoms such as H or F are preferred at para position. Finally, replacement of the phenyl ring by a pyridine affords a compound with similar potency, but with potentially better physicochemical properties which could constitute a new line of research for further studies. [-]
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Bioorganic & Medicinal Chemistry Letters, 2016, vol. 26, núm. 16Derechos de acceso
© 2016 Elsevier Ltd. All rights reserved.
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