Search

Your search keyword '"Cordeiro Da Silva, A."' showing total 8 results
Start Over Author "Cordeiro Da Silva, A." Journal european journal of medicinal chemistry
8 results on '"Cordeiro Da Silva, A."'

2. Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign

Author

Linciano, Pasquale, Cullia, Gregorio, Borsari, Chiara, Santucci, Matteo, Ferrari, Stefania, Witt, Gesa, Gul, Sheraz, Kuzikov, Maria, Ellinger, Bernhard, Santarém, Nuno, Cordeiro da Silva, Anabela, Conti, Paola, Bolognesi, Maria Laura, Roberti, Marinella, Prati, Federica, Bartoccini, Francesca, Retini, Michele, Piersanti, Giovanni, Cavalli, Andrea, Goldoni, Luca, Bertozzi, Sine Mandrup, Bertozzi, Fabio, Brambilla, Enzo, Rizzo, Vincenzo, Piomelli, Daniele, Pinto, Andrea, Bandiera, Tiziano, and Costi, Maria Paola

Published
2020
Full Text
View/download PDF

3. The discovery of aryl-2-nitroethyl triamino pyrimidines as anti-Trypanosoma brucei agents

Author

Linciano, Pasquale, primary, Pozzi, Cecilia, additional, Tassone, Giusy, additional, Landi, Giacomo, additional, Mangani, Stefano, additional, Santucci, Matteo, additional, Luciani, Rosaria, additional, Ferrari, Stefania, additional, Santarem, Nuno, additional, Tagliazucchi, Lorenzo, additional, Cordeiro-da-Silva, Anabela, additional, Tonelli, Michele, additional, Tondi, Donatella, additional, Bertarini, Laura, additional, Gul, Sheraz, additional, Witt, Gesa, additional, Moraes, Carolina B., additional, Costantino, Luca, additional, and Costi, Maria Paola, additional

Published
2023
Full Text
View/download PDF

4. Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics

Author

Borsari, Chiara, Jiménez-Antón, María Dolores, Eick, Julia, Bifeld, Eugenia, Torrado, Juan José, Olías-Molero, Ana Isabel, Corral, María Jesús, Santarem, Nuno, Baptista, Catarina, Severi, Leda, Gul, Sheraz, Wolf, Markus, Kuzikov, Maria, Ellinger, Bernhard, Reinshagen, Jeanette, Witt, Gesa, Linciano, Pasquale, Tait, Annalisa, Costantino, Luca, Luciani, Rosaria, Tejera Nevado, Paloma, Zander-Dinse, Dorothea, Franco, Caio H., Ferrari, Stefania, Moraes, Carolina B., Cordeiro-da-Silva, Anabela, Ponterini, Glauco, Clos, Joachim, Alunda, José María, and Costi, Maria Paola

Published
2019
Full Text
View/download PDF

5. Aryl thiosemicarbazones for the treatment of trypanosomatidic infections

Author

Linciano, Pasquale, Moraes, Carolina B., Alcantara, Laura M., Franco, Caio H., Pascoalino, Bruno, Freitas-Junior, Lucio H., Macedo, Sara, Santarem, Nuno, Cordeiro-da-Silva, Anabela, Gul, Sheraz, Witt, Gesa, Kuzikov, Maria, Ellinger, Bernhard, Ferrari, Stefania, Luciani, Rosaria, Quotadamo, Antonio, Costantino, Luca, and Costi, Maria Paola

Published
2018
Full Text
View/download PDF

6. Aryl thiosemicarbazones for the treatment of trypanosomatidic infections

Author

Maria Kuzikov, Gesa Witt, Bruno dos Santos Pascoalino, Caio Haddad Franco, Luca Costantino, Rosaria Luciani, Laura M. Alcantara, Nuno Santarém, Sara Macedo, Antonio Quotadamo, Lucio H. Freitas-Junior, Bernhard Ellinger, Carolina B. Moraes, Stefania Ferrari, Maria Paola Costi, Sheraz Gul, Anabela Cordeiro-da-Silva, Pasquale Linciano, and Publica

Subjects
Thiosemicarbazones, 0301 basic medicine, Trypanosoma, Stereochemistry, hERG, Antiprotozoal Agents, Trypanosoma brucei, 01 natural sciences, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Parasitic Sensitivity Tests, Thiadiazoles, Early-toxicity, Leishmania infantum, pan-anti-trypanosomatidic activity, Thiosemicarbazone, Trypanosoma cruzi, Pharmacology, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, parasitic diseases, Drug Discovery, medicine, Humans, Chagas Disease, Amastigote, Semicarbazone, Dose-Response Relationship, Drug, Molecular Structure, biology, Macrophages, General Medicine, biology.organism_classification, medicine.disease, 0104 chemical sciences, 3. Good health, 010404 medicinal & biomolecular chemistry, Mitochondrial toxicity, 030104 developmental biology, chemistry, biology.protein
Abstract

Basing on a library of thiadiazole derivatives showing anti-trypanosomatidic activity, we have considered the thiadiazoles opened forms and reaction intermediates, thiosemicarbazones, as compounds of interest for phenotypic screening against Trypanosoma brucei (Tb), intracellular amastigote form of Leishmania infantum (Li) and Trypanosoma cruzi (Tc). Similar compounds have already shown interesting activity against the same organisms. The compounds were particularly effective against T. brucei and T. cruzi. Among the 28 synthesized compounds, the best one was (E)-2-(4-((3.4-dichlorobenzyl)oxy)benzylidene) hydrazinecarbothioamide (A14) yielding a comparable anti-parasitic activity against the three parasitic species (TbEC50 = 2.31 mM, LiEC50 = 6.14 mM, TcEC50 = 1.31 mM) and a Selectivity Index higher than 10 with respect to human macrophages, therefore showing a pan-anti-trypanosomatidic activity. (E)-2-((3'.4'-dimethoxy-[1.1'-biphenyl]-3-yl)methyle ne) hydrazinecarbothioamide (A12) and (E)-2-(4-((3.4-dichlorobenzyl)oxy)benzylidene)hydrazine carbothioamide (A14) were able to potentiate the anti-parasitic activity of methotrexate (MTX) when evaluated in combination against T. brucei, yielding a 6-fold and 4-fold respectively Dose Reduction Index for MTX. The toxicity profile against four human cell lines and a panel of in vitro early-toxicity assays (comprising hERG, Aurora B, five cytochrome P450 isoforms and mitochondrial toxicity) demonstrated the low toxicity for the thosemicarbazones class in comparison with known drugs. The results confirmed thiosemicarbazones as a suitable chemical scaffold with potential for the development of properly decorated new anti-parasitic drugs.

Published
2018

7. Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds

Author

Borsari, Chiara, Santarem, Nuno, Torrado, Juan, Olías, Ana Isabel, Corral, María Jesús, Baptista, Catarina, Gul, Sheraz, Wolf, Markus, Kuzikov, Maria, Ellinger, Bernhard, Witt, Gesa, Gribbon, Philip, Reinshagen, Jeanette, Linciano, Pasquale, Tait, Annalisa, Costantino, Luca, Freitas-Junior, Lucio H., Moraes, Carolina B., Bruno dos Santos, Pascoalino, Alcântara, Laura Maria, Franco, Caio Haddad, Bertolacini, Claudia Danielli, Fontana, Vanessa, Tejera Nevado, Paloma, Clos, Joachim, Alunda, José María, Cordeiro-da-Silva, Anabela, Ferrari, Stefania, and Costi, Maria Paola

Published
2017
Full Text
View/download PDF

8. Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds

Author

Paloma Tejera Nevado, Maria Paola Costi, María Jesús Corral, Joachim Clos, Claudia Danielli Pereira Bertolacini, Caio Haddad Franco, Lucio H. Freitas-Junior, Vanessa Fontana, Markus Wolf, Annalisa Tait, Sheraz Gul, Gesa Witt, Juan J. Torrado, José María Alunda, Luca Costantino, Jeanette Reinshagen, Pasquale Linciano, Anabela Cordeiro-da-Silva, Nuno Santarém, Ana Isabel Olías, Bernhard Ellinger, Pascoalino Bruno dos Santos, Carolina B. Moraes, Philip Gribbon, Catarina Baptista, Maria Kuzikov, Laura M. Alcântara, Chiara Borsari, Stefania Ferrari, and Publica

Subjects
0301 basic medicine, Antiparasitic, medicine.drug_class, Stereochemistry, 02 engineering and technology, Trypanosoma brucei, 03 medical and health sciences, Mice, Chalcones, Cyclodextrins formulation, Early toxicity studies, Leishmania infantum, Trypanosoma cruzi, Animals, Antiparasitic Agents, Cell Line, Tumor, Cyclodextrins, Drug Carriers, Solubility, Trypanosomatina, Pharmacology, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, parasitic diseases, Drug Discovery, medicine, biology, Chemistry, General Medicine, 021001 nanoscience & nanotechnology, biology.organism_classification, Antiparasitic agent, 3. Good health, Bioavailability, 030104 developmental biology, 0210 nano-technology, Drug carrier
Abstract

Chalcones display a broad spectrum of pharmacological activities. Herein, a series of 2’-hydroxy methoxylated chalcones was synthesized and evaluated towards Trypanosoma brucei, Trypanosoma cruzi and Leishmania infantum. Among the synthesized library, compounds 1, 3, 4, 7 and 8 were the most potent and selective anti-T. brucei compounds (EC50 = 1.3–4.2 μM, selectivity index >10-fold). Compound 4 showed the best early-tox and antiparasitic profile. The pharmacokinetic studies of compound 4 in BALB/c mice using hydroxypropil-β-cyclodextrins formulation showed a 7.5 times increase in oral bioavailability.

Published
2016

Catalog

Books, media, physical & digital resources
See catalog results