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http://hdl.handle.net/10773/20720
Title: | N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials |
Author: | Gomes, Ana Machado, Marta Lobo, Lis Nogueira, Fatima Prudencio, Miguel Teixeira, Catia Gomes, Paula |
Keywords: | MALARIA-INFECTED ERYTHROCYTES PLASMODIUM-FALCIPARUM CHLOROQUINE ANALOGS PERMEABILITY DERIVATIVES INHIBITORS PARASITES GROWTH AGENTS |
Issue Date: | 2015 |
Publisher: | WILEY-V C H VERLAG GMBH |
Abstract: | In a follow-up study to our reports of N-cinnamoylated chloroquine and quinacrine analogues as promising dual-stage antimalarial leads with high in vitro potency against both blood-stage Plasmodium falciparum and liver-stage Plasmodium berghei, we decided to investigate the effect of replacing the cinnamoyl moiety with other acyl groups. Thus, a series of N-acylated analogues were synthesized, and their activities against blood- and liver-stage Plasmodiumspp. were assessed along with their in vitro cytotoxicities. Although the new N-acylated analogues were found to be somewhat less active and more cytotoxic than their N-cinnamoylated counterparts, they equally displayed nanomolar activities in vitro against blood-stage drug-sensitive and drug-resistant P.falciparum, and significant in vitro liver-stage activity against P.berghei. Therefore, it is demonstrated that simple N-acylated surrogates of classical antimalarial drugs are promising dual-stage antimalarial leads. |
Peer review: | yes |
URI: | http://hdl.handle.net/10773/20720 |
DOI: | 10.1002/cmdc.201500164 |
ISSN: | 1860-7179 |
Publisher Version: | 10.1002/cmdc.201500164 |
Appears in Collections: | CICECO - Artigos |
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File | Description | Size | Format | |
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N-Cinnamoylation of Antimalarial Classics Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials_10.1002cmdc.201500164.pdf | 763.89 kB | Adobe PDF |
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