Synthesis and antiprotozoal activity of furanchalcone–quinoline, furanchalcone–chromone and furanchalcone–imidazole hybrids
Impact
Scholar |
Other documents of the author: García, Elisa; Coa, Juan Carlos; Otero, Elver; Carda, Miguel; Vélez, Iván D.; Robledo, Sara M.; Cardona Galeano, Wilson Isidro
Metadata
Show full item recordcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
comunitat-uji-handle4:
INVESTIGACIONThis resource is restricted
https://doi.org/10.1007/s00044-017-2076-6 |
Metadata
Title
Synthesis and antiprotozoal activity of furanchalcone–quinoline, furanchalcone–chromone and furanchalcone–imidazole hybridsAuthor (s)
Date
2018Publisher
Springer VerlagISSN
1054-2523; 1554-8120Bibliographic citation
García, E., Coa, J.C., Otero, E. et al. Med Chem Res (2018) 27: 497. https://doi.org/10.1007/s00044-017-2076-6Type
info:eu-repo/semantics/articlePublisher version
https://link.springer.com/article/10.1007/s00044-017-2076-6Version
info:eu-repo/semantics/publishedVersionSubject
Abstract
We report herein the synthesis and biological activities (cytotoxicity, leishmanicidal, and trypanocidal) of several furanchalcone–quinoline, furanchalcone–chromone, and furanchalcone–imidazole hybrids. The synthesized ... [+]
We report herein the synthesis and biological activities (cytotoxicity, leishmanicidal, and trypanocidal) of several furanchalcone–quinoline, furanchalcone–chromone, and furanchalcone–imidazole hybrids. The synthesized compounds were evaluated against amastigotes forms of L. (V) panamensis, which is the most prevalent Leishmania species in Colombia and against Trypanosoma cruzi, which is the major pathogenic species to humans. Cytotoxicity was evaluated against human U-937 macrophages. Compounds (6e, 8a–8f, 11b, and 11c) were active against both L. (V) panamensis and T. cruzi being 8e and 8f the most active compounds with an EC50 of 0.78 and 2.16 µM against L. (V) panamensis, respectively, and 0.66 and 0.72 µM against T. cruzi, respectively. Seven hybrid compounds showed better activity than meglumine antimoniate and the anti-trypanosomal activity of nine compounds were higher than benznidazole. Although these compounds showed toxicity for mammalian U-937 cells, they still have the potential to be considered as candidates for antileishmanial or trypanocydal drug development. There is not a clear relationship between the antiprotozoal activity and the length of the alkyl linker. However, we obtained higher bioactivity when the alkyl linker has nine and twelve carbon atoms. Furanchalcone-imidazole hybrids were the most active of all compounds, showing that the imidazole salt moiety is important for their biological actions. [-]
Is part of
Med Chem Res (2018) 27Investigation project
grant CODI 6203 and CIDEPRORights
http://rightsstatements.org/vocab/CNE/1.0/
info:eu-repo/semantics/restrictedAccess
info:eu-repo/semantics/restrictedAccess
This item appears in the folowing collection(s)
- QUIO_Articles [690]