Please use this identifier to cite or link to this item:
https://hdl.handle.net/10216/82064
Author(s): | Nuno Vale Joana Matos Jiri Gut Fatima Nogueira Virgilio do Rosario Philip J Rosenthal Rui Moreira Paula Gomes |
Title: | Imidazolidin-4-one peptidomimetic derivatives of primaquine: Synthesis and antimalarial activity |
Issue Date: | 2008 |
Abstract: | The synthesis of imidazolidin-4-one derivatives of primaquine containing the five-membered ring at the C-terminus of a dipeptide backbone coupled to the parent drug is described. These peptidomimetic derivatives were active against a chloroquine-resistant Plasmodium falciparum strain and inhibited the development of the sporogonic cycle of Plasmodium berghei, affecting the appearance of oocysts in the midguts of the mosquitoes. The novel imidazolidin-4-ones are extremely stable, both in human plasma and in pH 7.4 buffer, as a result of N(1)-acylation. Thus, 'internal' imidazolidin-4-ones derived from dipeptidyl 8-aminoquinolines represent a new entry in antimalarial structure-activity relationships. |
Subject: | Química Chemical sciences |
Scientific areas: | Ciências exactas e naturais::Química Natural sciences::Chemical sciences |
URI: | https://hdl.handle.net/10216/82064 |
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 |
This item is licensed under a Creative Commons License