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https://www.arca.fiocruz.br/handle/icict/26872
PHTHALOYL AMINO ACIDS AS ANTI-INFLAMMATORY AND IMMUNOMODULATORY PROTOTYPES
Author
Leite, Ana Cristina Lima
Barbosa, Fábio Fernandes
Cardoso, Marcos Veríssimo de Oliveira
Moreira, Diogo Rodrigo de Magalhães
Coêlho, Lucas Cunha Duarte
Silva, Elany Barbosa da
Oliveira Filho, Gevanio Bezerra de
Souza, Valdênia Maria Oliveira de
Pereira, Valéria Rêgo A
Reis, Luiza de Campos
Ferreira, Paulo Michel Pinheiro
Pessoa, Claudia
Wanderley, Almir Gonçalves
Mota, Fernanda Virgínia Barreto
Silva, Teresinha Gonçalves da
Barbosa, Fábio Fernandes
Cardoso, Marcos Veríssimo de Oliveira
Moreira, Diogo Rodrigo de Magalhães
Coêlho, Lucas Cunha Duarte
Silva, Elany Barbosa da
Oliveira Filho, Gevanio Bezerra de
Souza, Valdênia Maria Oliveira de
Pereira, Valéria Rêgo A
Reis, Luiza de Campos
Ferreira, Paulo Michel Pinheiro
Pessoa, Claudia
Wanderley, Almir Gonçalves
Mota, Fernanda Virgínia Barreto
Silva, Teresinha Gonçalves da
Affilliation
Múltipla – ver em Notas
Abstract
Abstract A series of phthalimide analogs were synthesized
by derivatization of phthalic anhydride, a highly toxic substance,
using a ‘‘one pot’’ condensation reaction to a-amino
acids. All phthaloyl amino acid derivatives presented anti-oral
inflammatory activity, but compounds 2e and 2g were found
to possess the best activities comparable to thalidomide.Most
of the compounds effectively suppressed nitric oxide production
inmurine cells stimulatedwith lipopolysaccharide.Nphthaloyl
amino acids did not exhibit any significant cytotoxicity
in vitro when tested against tumor cells as well as a
spleen cell culture of BALB/c mice. Compounds 2a, 2g, and
2h were able to inhibit TNF-a and IL-1b production by
macrophages. At the same concentration, thalidomide did not
exhibit significant inhibitory activity.
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