Please use this identifier to cite or link to this item:
https://hdl.handle.net/10216/82125
Author(s): | Ana Gomes Marta Machado Lis Lobo Fatima Nogueira Miguel Prudencio Catia Teixeira Paula Gomes |
Title: | N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials |
Issue Date: | 2015 |
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. |
Subject: | Medicina básica Basic medicine |
Scientific areas: | Ciências médicas e da saúde::Medicina básica Medical and Health sciences::Basic medicine |
URI: | https://hdl.handle.net/10216/82125 |
Document Type: | Artigo em Revista Científica Internacional |
Rights: | openAccess |
License: | https://creativecommons.org/licenses/by-nc/4.0/ |
Appears in Collections: | FCUP - Artigo em Revista Científica Internacional |
Files in This Item:
File | Description | Size | Format | |
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109312.pdf | 1.69 MB | Adobe PDF | View/Open | |
109312.1.pdf | 1.69 MB | Adobe PDF | View/Open |
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