8 documents found, page 1 of 1
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, GillesToxoplasmosis 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 (HDAC) inhibitor we previously synthesized, named JF363, to act in vitro against a large panel of Toxoplasma strains, as well as against the liver and blood stages of Plasmodium parasites, the causative agents of malaria. In vivo administra...
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)...
Synthesis and antiplasmodial activity of regioisomers and epimers of second-gen...
Singh, Lovepreet; Fontinha, Diana; Francisco, Denise; Prudêncio, Miguel; Singh, KamaljitWith its strong effect on vector-borne diseases, and insecticidal effect on mosquito vectors of malaria, inhibition of sporogonic and blood-stage development of Plasmodium falciparum, as well as in vitro and in vivo impairment of the P. berghei development inside hepatocytes, ivermectin (IVM) continues to represent an antimalarial therapeutic worthy of investigation. The in vitro activity of the first-generatio...
Synthesis and structure-activity relationships of new chiral spiro-β-lactams hi...
Alves, Nuno Guerreiro; Bártolo, Inês; Alves, Américo J. S.; Fontinha, Diana; Francisco, Denise; Lopes, Susana M. M.; Soares, Maria I. L.The synthesis and antimicrobial activity of new spiro-β-lactams is reported. The design of the new molecules was based on the structural modulation of two previously identified lead spiro-penicillanates with dual activity against HIV and Plasmodium. The spiro-β-lactams synthesized were assayed for their in vitro activity against HIV-1, providing relevant structure-activity relationship information. Among the te...
Spiro-β-lactam BSS-730A Displays Potent Activity against HIV and Plasmodium
Bártolo, Inês; Santos, Bruna S; Fontinha, Diana; Machado, Marta; Francisco, Denise; Sepodes, Bruno; Rocha, João; Mota-Filipe, Hélder; Pinto, RuiThe high burden of malaria and HIV/AIDS prevents economic and social progress in developing countries. A continuing need exists for development of novel drugs and treatment regimens for both diseases in order to address the tolerability and long-term safety concerns associated with current treatment options and the emergence of drug resistance. We describe new spiro-β-lactam derivatives with potent (nM) activit...
Spiro-ß-lactam BSS-730A Displays Potent Activity against HIV and Plasmodium
Bártolo, Inês; Santos, Bruna S.; Fontinha, Diana; Machado, Marta; Francisco, Denise; Sepodes, Bruno; Rocha, Joao; Mota-Filipe, Hélder; Pinto, RuiThe high burden of malaria and HIV/AIDS prevents economic and social progress in developing countries. A continuing need exists for development of novel drugs and treatment regimens for both diseases in order to address the tolerability and long-term safety concerns associated with current treatment options and the emergence of drug resistance. We describe new spiro-β-lactam derivatives with potent (nM) activit...
Synthesis and structure-activity relationships of new chiral spiro-ß-lactams hi...
G. Alves, Nuno; Bártolo, Inês; Alves, Américo; Fontinha, Diana; Francisco, Denise; Lopes, Susana M. M.; Soares, Maria I. L.; Simões, Carlos J. V.The synthesis and antimicrobial activity of new spiro-β-lactams is reported. The design of the new molecules was based on the structural modulation of two previously identified lead spiro-penicillanates with dual activity against HIV and Plasmodium. The spiro-β-lactams synthesized were assayed for their in vitro activity against HIV-1, providing relevant structure-activity relationship information. Among the te...
Synthesis and structure-activity relationships of new chiral spiro-β-lactams hi...
Alves, Nuno Guerreiro; Bártolo, Inês; Alves, Américo J.S.; Fontinha, Diana; Francisco, Denise; Lopes, Susana M.M.; Soares, Maria I.L.The synthesis and antimicrobial activity of new spiro-β-lactams is reported. The design of the new molecules was based on the structural modulation of two previously identified lead spiro-penicillanates with dual activity against HIV and Plasmodium. The spiro-β-lactams synthesized were assayed for their in vitro activity against HIV-1, providing relevant structure-activity relationship information. Among the te...