12 documents found, page 1 of 2
Surface-active ionic liquids derived from antimalarial drugs and natural lipids...
Ferraz, Ricardo; Silva, Ana Teresa; Oliveira, Isabel S.; Duarte, Denise; Moita, Diana; Nogueira, Fátima; Prudêncio, Miguel; Gomes, PaulaThe use of Ionic Liquids (ILs) in Medicinal and Pharmaceutical Chemistry has been greatly evolving since they were first used as alternative solvents for the chemical synthesis of active pharmaceutical ingredients (APIs). ILs are now used with other purposes in this area, such as adjuvants in drug formulation and delivery, or even as bioactive compounds per se. New ionic structures with biologically relevant pr...
Whole-sporozoite malaria vaccines: where we are, where we are going
Moita, Diana; Prudêncio, MiguelThe malaria vaccination landscape has seen significant advancements with the recent endorsement of RTS,S/AS01 and R21/Matrix-M vaccines, which target the pre-erythrocytic stages of Plasmodium falciparum (Pf) infection. However, several challenges remain to be addressed, including the incomplete protection afforded by these vaccines, their dependence on a single Pf antigen, and the fact that they were not design...
SARS-CoV-2 decreases malaria severity in co-infected rodent models
Fraga, Ana; Mósca, Andreia F.; Moita, Diana; Simas, J. Pedro; Nunes-Cabaço, Helena; Prudêncio, MiguelCoronavirus disease 2019 (COVID-19) and malaria, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and Plasmodium parasites, respectively, share geographical distribution in regions where the latter disease is endemic, leading to the emergence of co-infections between the two pathogens. Thus far, epidemiologic studies and case reports have yielded insufficient data on the reciprocal impact ...
Combining natural bile acids with old basic drugs affords new triple stage anti...
Silva, Ana Teresa; Oliveira, Isabel; Duarte, Denise; Moita, Diana; Prudêncio, Miguel; Nogueira, Fátima; Ferraz, Ricardo; Marques, Eduardo F.Ionic liquids (ILs) are special organic salts that have been gaining momentum in medicinal chemistry. Despite their simple and cost-effective synthesis, ILs offer an easy access to structures of biological interest by combining bioactive molecules with opposite polarities, e.g., via simple ionic pairing of an acid with a base. This makes ILs of special interest for treating malaria. Since this disease is preval...
The effect of dosage on the protective efficacy of whole-sporozoite formulation...
Moita, Diana; Rôla, Catarina; Nunes-Cabaço, Helena; Nogueira, Gonçalo; Maia, Teresa G.; Othman, Ahmad Syibli; Franke-Fayard, Blandine; Janse, Chris J.Immunization with Plasmodium sporozoites, either attenuated or administered under the cover of an antimalarial drug, can induce strong protection against malaria in pre-clinical murine models, as well as in human trials. Previous studies have suggested that whole-sporozoite (WSpz) formulations based on parasites with longer liver stage development induce higher protection, but a comparative analysis of four dif...
New 4-(N-cinnamoylbutyl)aminoacridines as potential multi-stage antiplasmodial ...
Fonte, Mélanie; Fontinha, Diana; Moita, Diana; Caño-Prades, Omar; Avalos-Padilla, Yunuen; Fernàndez-Busquets, Xavier; Prudêncio, Miguel; Gomes, PaulaA novel family of 4-aminoacridine derivatives was obtained by linking this heteroaromatic core to different trans-cinnamic acids. The 4-(N-cinnamoylbutyl)aminoacridines obtained exhibited in vitro activity in the low- or sub-micromolar range against (i) hepatic stages of Plasmodium berghei, (ii) erythrocytic forms of Plasmodium falciparum, and (iii) early and mature gametocytes of Plasmodium falciparum. The mos...
Synthesis od new surface-active ionic liquids derived from antimalarial drugs a...
Silva, Ana Teresa; Oliveira, Isabel; Duarte, Denise; Moita, Diana; Prudêncio, Miguel; Nogueira, Fátima; Teixeira, Cátia; Ferraz, RicardoMalaria is a parasitic disease that occurs mostly in low-income countries, thus its containment or, ultimately, eradication demands new methodologies and synthetic strategies that are simple and inexpensive. Ionic liquids (ILs) may assume a prominent role in this scenario, as they are catching the attention of the Medicinal Chemistry community owing to their intrinsic biological activity and affordable synthesi...
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent a...
Poje, Goran; Pessanha de Carvalho, Lais; Held, Jana; Moita, Diana; Prudêncio, Miguel; Perković, Ivana; Tandarić, Tana; Vianello, Robert; Rajić, ZrinkaMalaria remains one of the major health problems worldwide. The lack of an effective vaccine and the increasing resistance of Plasmodium to the approved antimalarial drugs demands the development of novel antiplasmodial agents that can effectively prevent and/or treat this disease. Harmiquins represent hybrids that combine two moieties with different mechanisms of antiplasmodial activity in one molecule, i.e., ...
The protein aggregation inhibitor YAT2150 has potent antimalarial activity in P...
Bouzón-Arnáiz, Inés; Avalos-Padilla, Yunuen; Biosca, Arnau; Caño-Prades, Omar; Román-Álamo, Lucía; Valle, Javier; Andreu, David; Moita, DianaBackground: By 2016, signs of emergence of Plasmodium falciparum resistance to artemisinin and partner drugs were detected in the Greater Mekong Subregion. Recently, the independent evolution of artemisinin resistance has also been reported in Africa and South America. This alarming scenario calls for the urgent development of new antimalarials with novel modes of action. We investigated the interference with p...
A genetically modified Plasmodium berghei parasite as a surrogate for whole-spo...
Moita, Diana; Maia, Teresa G.; Duarte, Miguel; Andrade, Carolina M.; Albuquerque, Inês S.; Dwivedi, Ankit; Silva, Joana C.; González-Céron, LiliaTwo malaria parasite species, Plasmodium falciparum (Pf) and P. vivax (Pv) are responsible for most of the disease burden caused by malaria. Vaccine development against this disease has focused mainly on Pf. Whole-sporozoite (WSp) vaccination, targeting pre-erythrocytic (PE) parasite stages, is a promising strategy for immunization against malaria and several PfWSp-based vaccine candidates are currently undergo...