8 documents found, page 1 of 1
Improving the antimycobacterial drug Clofazimine through formation of organic s...
Bento, Clara M.; Silva, Ana Teresa; Mansano, Bruno; Aguiar, Luísa; Teixeira, Cátia; Gomes, Maria Salomé; Gomes, Paula; Silva, Tânia; Ferraz, RicardoThis work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutical ingredients (API-OSs), as those herein disclosed, hold promise as cost-effective formulations with improved fea...
Boosting cosmeceutical peptides: coupling imidazolium-based ionic liquids to pe...
Gomes, Ana; Bessa, Lucinda J.; Fernandes, Iva; Aguiar, Luísa; Ferraz, Ricardo; Monteiro, Cláudia; Martins, M. Cristina L.; Mateus, Nuno; Gameiro, PaulaFollowing our previous reports on dual-action antibacterial and collagenesis-inducing hybrid peptide constructs based on “pentapeptide-4” (PP4, with amino acid sequence KTTKS), whose N-palmitoyl derivative is the well-known cosmeceutical ingredient Matrixyl, herein we disclose novel ionic liquid/PP4 conjugates (IL-KTTKS). These conjugates present potent activity against either antibiotic-susceptible strains or ...
Drug‐derived surface‐active ionic liquids: a cost‐effective way to expressively...
Silva, Ana Teresa; Oliveira, Isabel S.; Gomes, Joana; Aguiar, Luísa; Fontinha, Diana; Duarte, Denise; Nogueira, Fátima; Prudêncio, Miguel© 2021 Wiley-VCH GmbH; Inspired by previous disclosure of room-temperature ionic liquids derived from primaquine and cinnamic acids, which displayed slightly enhanced blood-stage activity compared to the parent drug, we have now combined this emblematic antimalarial with natural fatty acids. This affords surface-active ionic liquids whose liver-stage antiplasmodial activity is either retained or slightly enhanc...
Drug-derived surface-active ionic liquids: a cost-effective way to expressively...
Silva, Ana Teresa; Oliveira, Isabel S.; Gomes, Joana; Aguiar, Luísa; Fontinha, Diana; Duarte, Denise; Nogueira, Fátima; Prudêncio, MiguelInspired by previous disclosure of room-temperature ionic liquids derived from primaquine and cinnamic acids, which displayed slightly enhanced blood-stage activity compared to the parent drug, we have now combined this emblematic antimalarial with natural fatty acids. This affords surface-active ionic liquids whose liver-stage antiplasmodial activity is either retained or slightly enhanced, while revealing blo...
The emerging role of ionic liquid-based approaches for enhanced skin permeation...
Gomes, Ana; Aguiar, Luísa; Ferraz, Ricardo; Teixeira, Cátia; Gomes, PaulaTopical and transdermal delivery systems are of undeniable significance and ubiquity in healthcare, to facilitate the delivery of active pharmaceutical ingredients, respectively, onto or across the skin to enter systemic circulation. From ancient ointments and potions to modern micro/nanotechnological devices, a variety of approaches has been explored over the ages to improve the skin permeation of diverse medi...
Cinnamic acid conjugates in the rescuing and repurposing of classical antimalar...
Silva, Ana Teresa; Bento, Clara M.; Pena, Ana C.; Figueiredo, Luísa M.; Prudêncio, Cristina; Aguiar, Luísa; Silva, Tânia; Ferraz, RicardoCinnamic acids are compounds of natural origin that can be found in many different parts of a wide panoply of plants, where they play the most diverse biological roles, often in a conjugated form. For a long time, this has been driving Medicinal Chemists towards the investigation of the therapeutic potential of natural, semi-synthetic, or fully synthetic cinnamic acid conjugates. These efforts have been steadil...
Coupling the cell-penetrating peptides transportan and transportan 10 to primaq...
Aguiar, Luísa; Machado, Marta; Sanches-Vaz, Margarida; Prudêncio, Miguel; Vale, Nuno; Gomes, PaulaThis journal is © The Royal Society of Chemistry 2018; Novel primaquine-cell penetrating peptide conjugates were synthesised and tested in vitro against liver stage Plasmodium berghei parasites. Generally, the conjugates were more active than the parent peptides and, in some cases, than the parent drug. These are unprecedented findings that may open a new route towards antimalarial drug rescuing.; The authors a...
Cinnamic acid conjugates in the rescuing and repurposing of classical antimalar...
Silva, Ana Teresa; Bento, Clara M.; Pena, Ana C; Figueiredo, Luisa M.; Prudêncio, Cristina; Aguiar, Luísa; Silva, Tânia; Ferraz, Ricardo© 2019 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 (http://creativecommons.org/licenses/by/4.0/).; Cinnamic acids are compounds of natural origin that can be found in many different parts of a wide panoply of plants, where they play the most diverse biological roles, often...