58 documents found, page 1 of 6
Unexpected rearrangement of ivermectin in the synthesis of new derivatives with...
Sulik, Michał; Fontinha, Diana; Steverding, Dietmar; Sobczak, Szymon; Antoszczak, Michał; Prudêncio, Miguel; Huczyński, Adam© 2023 The Authors. Published by Elsevier Masson SAS. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).; Ivermectin is a sixteen-membered macrolactone "wonder drug" of Nobel prize-honored distinction that exhibits a wide range of antiparasitic activities. It has been used for almost four decades in the treatment of various parasitic diseases in hum...
Facile access to structurally diverse antimalarial indoles using a one‐pot A3 c...
Silva, Gustavo Da; Luz, André F. S.; Duarte, Denise; Fontinha, Diana; Silva, Vera L. M.; Almeida Paz, Filipe A.; Madureira, Ana Margarida© 2023 Wiley-VCH GmbH; A multistep and diversity-oriented synthetic route aiming at the A3 coupling/domino cyclization of o-ethynyl anilines, aldehydes and s-amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross-coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomp...
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, Paula© 2023 The Authors. Published by Elsevier Masson SAS. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).; A 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) hep...
Design, synthesis and antiplasmodial evaluation of new amide-, carbamate-, and ...
Marinović, Marina; Rimac, Hrvoje; de Carvalho, Lais Pessanha; Rôla, Catarina; Santana, Sofia; Pavić, Kristina; Held, Jana; Prudêncio, Miguel© 2023 Elsevier Ltd. All rights reserved.; Malaria, one of the oldest parasitic diseases, remains a global health threat, and the increasing resistance of the malaria parasite to current antimalarials is forcing the discovery of new, effective drugs. Harmicines, hybrid compounds in which harmine/β-carboline alkaloids and cinnamic acid derivatives are linked via an amide bond or a triazole ring, represent new an...
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.© The Author(s) 2023. Open Access. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party...
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 ...
Facile Access to Structurally Diverse Antimalarial Indoles Using a One-Pot A3 C...
da Silva, Gustavo; Luz, André F. S.; Duarte, Denise; Fontinha, Diana; Silva, Vera L. M.; Almeida Paz, Filipe A.; Madureira, Ana M.; Simões, SandraA multistep and diversity-oriented synthetic route aiming at the A3 coupling/domino cyclization of o-ethynyl anilines, aldehydes and s-amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross-coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomponent reaction underwen...
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, Diana© The Author(s) 2022. Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party ...
Translation of liver stage activity of M5717, a Plasmodium elongation factor 2 ...
Khandelwal, Akash; Arez, Francisca; Alves, Paula M.; Badolo, Lassina; Brito, Catarina; Fischli, Christoph; Fontinha, Diana; Oeuvray, Claude© The Author(s) 2022. Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party ...
A Histone Deacetylase (HDAC) inhibitor with pleiotropic in vitro anti-toxoplasm...
Jublot, Delphine; Cavaillès, Pierre; Kamche, Salima; Francisco, Denise; Fontinha, Diana; Prudêncio, Miguel; Guichou, Jean-Francois; Labesse, Gilles© 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).; Toxoplasmosis is a highly prevalent human disease, and virulent strains of this parasite emerge from wild biotopes. Here, we report on the potential of a histone deacetylase...