Design, synthesis and antimalarial evaluation of novel thiazole derivatives
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http://dx.doi.org/10.1016/j.bmcl.2016.07.010 |
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Title
Design, synthesis and antimalarial evaluation of novel thiazole derivativesAuthor (s)
Date
2016Publisher
ElsevierISSN
0960-894XBibliographic citation
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.Type
info:eu-repo/semantics/articlePublisher version
http://bs8lz6ys5q.search.serialssolutions.com/?ctx_ver=Z39.88-2004&ctx_enc=info% ...Subject
Abstract
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. 16Rights
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