34 documents found, page 1 of 4
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...
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...
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...
Pre-erythrocytic activity of M5717 in monotherapy and combination in preclinica...
Fontinha, Diana; Arez, Francisca; Gal, Isabella Ramella; Nogueira, Gonçalo; Moita, Diana; Baeurle, Tobias Hyun Ho; Brito, Catarina; Spangenberg, ThomasCopyright © 2022 The Authors. Published by American Chemical Society; Combination therapies have emerged to mitigate Plasmodium drug resistance, which has hampered the fight against malaria. M5717 is a potent multistage antiplasmodial drug under clinical development, which inhibits parasite protein synthesis. The combination of M5717 with pyronaridine, an inhibitor of hemozoin formation, displays potent activit...
Discovery of spirooxadiazoline oxindoles with dual-stage antimalarial activity
Lopes, Elizabeth A.; Mestre, Raquel; Fontinha, Diana; Legac, Jenny; Pei, Jinxin V.; Sanches-Vaz, Margarida; Mori, Mattia; Lehane, Adele M.© 2022 Published by Elsevier Masson SAS.; Malaria remains a prevalent infectious disease in developing countries. The first-line therapeutic options are based on combinations of fast-acting artemisinin derivatives and longer-acting synthetic drugs. However, the emergence of resistance to these first-line treatments represents a serious risk, and the discovery of new effective drugs is urgently required. For thi...
Unveiling a family of spiro-ß-lactams with anti-HIV and antiplasmodial activity...
Alves, Américo; Alves, Nuno G.; Bártolo, Inês; Fontinha, Diana; Caetano, Soraia; Prudêncio, Miguel; Taveira, Nuno; Melo, Teresa M. V. D. Pinho EThe molecular architecture of spirocyclic compounds has been widely explored within the medicinal chemistry field to obtain new compounds with singular three-dimensional pharmacophoric features and improved bioactivity. Herein, the synthesis of 68 new spirocyclopentene-β-lactams is described, resulting from a rational drug design and structural modulation of a highly promising lead compound BSS-730A, previously...
Broad Spectrum Functional Activity of Structurally Related Monoanionic Au(III) ...
Le Gal, Yann; Filatre-Furcate, Agathe; Lorcy, Dominique; Jeannin, Olivier; Roisnel, Thierry; Dorcet, Vincent; Fontinha, Diana; Francisco, DeniseThe biological properties of sixteen structurally related monoanionic gold (III) bis(dithiolene/diselenolene) complexes were evaluated. The complexes differ in the nature of the heteroatom connected to the gold atom (AuS for dithiolene, AuSe for diselenolene), the substituent on the nitrogen atom of the thiazoline ring (Me, Et, Pr, iPr and Bu), the nature of the exocyclic atom or group of atoms (O, S, Se, C(CN)...