| Author | Carrara, Vanessa da Silva | |
| Author | Cunha Júnior, Edézio Ferreira | |
| Author | Santos, Eduardo Caio Torres | |
| Author | Corrêa, Arlene Gonçalves | |
| Author | Monteiro, Júlia L. | |
| Author | Demarchi, Izabel Galhardo | |
| Author | Lonardoni, Maria Valdinez Campana | |
| Author | Cortez, Diógenes Aparício Garcia | |
| Access date | 2015-08-19T13:49:28Z | |
| Available date | 2015-08-19T13:49:28Z | |
| Document date | 2013 | |
| Citation | CARRARA, Vanessa da Silva; Antileishmanial activity of amides from Piper 23(3): 447-454, May/Jun. 2013 amalago and synthetic analogs. Revista Brasileira de Farmacognosia, v.23, n.3, p.447-454, maio/jun. 2013. | pt_BR |
| ISSN | 0102-695X | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/11532 | |
| Language | eng | pt_BR |
| Publisher | Universidade Federal do Paraná, Laboratório de Farmacognosia | pt_BR |
| Rights | open access | |
| Title | Antileishmanial activity of amides from Piper amalago and synthetic analogs | pt_BR |
| Type | Article | |
| DOI | 10.1590/S0102-695X2013005000022 | pt_BR |
| Abstract | Two natural amides isolated from the chloroform extract of Piper amalago
L., Piperaceae, leaves, a hydrogenated derivative and seven synthetic analogs were
tested against the promastigote and intracellular amastigote forms of Leishmania
amazonensis. The antileishmanial activity was evaluated in terms of growth inhibitory
concentration for 50% of protozoa (IC50). The cytotoxicity toward the J774A1
macrophages was evaluated in terms of the cytotoxic concentrations for 50% of
macrophages (CC50). The ability to induce nitric oxide production was also investigated
for all compounds. The saturated amide 7-(1,3-benzodioxol-5-yl)-1-(1-pyrrolidinyl)-
1-heptanone was obtained by hydrogenation of the natural compound N-[7-(3’,4’-
methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl]pyrrolidine. Synthetic amides were
prepared by addition of the appropriate amine to the corresponding acyl chloride.
The natural compound, N-[7-(3’,4’-methylenedioxyphenyl)-2(E),4(E)-heptadienoyl]
pyrrolidine, was the most active of all tested compounds against the promastigote and
intracellular amastigote forms with IC50 values of 15 μM and 14.5 μM, respectively.
None of the compounds modulated the production of nitric oxide. | pt_BR |
| Affilliation | Universidade Estadual de Maringá. Departamento de Farmácia. Maringá, PR, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil. | pt_BR |
| Affilliation | Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil. | pt_BR |
| Affilliation | Universidade Estadual de Maringá. Departamento de Análises Clínicas. Maringá, PR, Brasil. | pt_BR |
| Affilliation | Universidade Estadual de Maringá. Departamento de Análises Clínicas. Maringá, PR, Brasil. | pt_BR |
| Affilliation | Universidade Estadual de Maringá. Departamento de Farmácia. Maringá, PR, Brasil. | pt_BR |
| Subject | Amides | pt_BR |
| Subject | Antileishmanial activity | pt_BR |
| Subject | Piper amalago | pt_BR |
| Subject | Synthetic analogs | pt_BR |
| DeCS | Amidas | pt_BR |
| DeCS | Compostos Orgânicos | pt_BR |
| DeCS | Leishmania amazonensis | pt_BR |
