Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives
This paper describes the preparation of N,N'-disubstituted ethylenediamine and imidazolidine derivatives and their in vitro biological activities against Leishmania species. Of the nine synthesized compounds, five displayed a good activity in both L. amazonensis and L. major promastigotes. The...
Saved in:
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Wiley
2010-01-01
|
| Series: | The Scientific World Journal |
| Online Access: | http://dx.doi.org/10.1100/tsw.2010.176 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832564508490465280 |
|---|---|
| author | Gustavo S. G. de Carvalho Patrícia A. Machado Daniela T. S. de Paula Elaine S. Coimbra Adilson D. da Silva |
| author_facet | Gustavo S. G. de Carvalho Patrícia A. Machado Daniela T. S. de Paula Elaine S. Coimbra Adilson D. da Silva |
| author_sort | Gustavo S. G. de Carvalho |
| collection | DOAJ |
| description | This paper describes the preparation of N,N'-disubstituted ethylenediamine and imidazolidine derivatives and their in vitro biological activities against Leishmania species. Of the nine synthesized compounds, five displayed a good activity in both L. amazonensis and L. major promastigotes. The compounds 1,2-Bis(p-methoxybenzyl)ethylenediamine (4) and 1,3-Bis(p-methoxybenzyl)imidazolidines (5) showed the best activity on intracellular amastigotes, with IC50 values of 2.0 and 9.4 μ/mL, respectively. In addition, none of compounds were cytotoxic against mammalian cells. The leishmanicidal activity can be related with inhibition of polyamine synthesis and cellular penetration within biological membranes. |
| format | Article |
| id | doaj-art-df5b223bc47b45b4baed8cc32ea7f8f3 |
| institution | Kabale University |
| issn | 1537-744X |
| language | English |
| publishDate | 2010-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | The Scientific World Journal |
| spelling | doaj-art-df5b223bc47b45b4baed8cc32ea7f8f32025-02-03T01:10:56ZengWileyThe Scientific World Journal1537-744X2010-01-01101723173010.1100/tsw.2010.176Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine DerivativesGustavo S. G. de Carvalho0Patrícia A. Machado1Daniela T. S. de Paula2Elaine S. Coimbra3Adilson D. da Silva4Departamento de Química, I.C.E., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, Minas Gerais, BrazilDepartamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, Minas Gerais, BrazilDepartamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, Minas Gerais, BrazilDepartamento de Parasitologia, Microbiologia e Imunologia, I.C.B., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, Minas Gerais, BrazilDepartamento de Química, I.C.E., Universidade Federal de Juiz de Fora, Cidade Universitária, Juiz de Fora, Minas Gerais, BrazilThis paper describes the preparation of N,N'-disubstituted ethylenediamine and imidazolidine derivatives and their in vitro biological activities against Leishmania species. Of the nine synthesized compounds, five displayed a good activity in both L. amazonensis and L. major promastigotes. The compounds 1,2-Bis(p-methoxybenzyl)ethylenediamine (4) and 1,3-Bis(p-methoxybenzyl)imidazolidines (5) showed the best activity on intracellular amastigotes, with IC50 values of 2.0 and 9.4 μ/mL, respectively. In addition, none of compounds were cytotoxic against mammalian cells. The leishmanicidal activity can be related with inhibition of polyamine synthesis and cellular penetration within biological membranes.http://dx.doi.org/10.1100/tsw.2010.176 |
| spellingShingle | Gustavo S. G. de Carvalho Patrícia A. Machado Daniela T. S. de Paula Elaine S. Coimbra Adilson D. da Silva Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives The Scientific World Journal |
| title | Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives |
| title_full | Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives |
| title_fullStr | Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives |
| title_full_unstemmed | Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives |
| title_short | Synthesis, Cytotoxicity, and Antileishmanial Activity of N,N'-Disubstituted Ethylenediamine and Imidazolidine Derivatives |
| title_sort | synthesis cytotoxicity and antileishmanial activity of n n disubstituted ethylenediamine and imidazolidine derivatives |
| url | http://dx.doi.org/10.1100/tsw.2010.176 |
| work_keys_str_mv | AT gustavosgdecarvalho synthesiscytotoxicityandantileishmanialactivityofnndisubstitutedethylenediamineandimidazolidinederivatives AT patriciaamachado synthesiscytotoxicityandantileishmanialactivityofnndisubstitutedethylenediamineandimidazolidinederivatives AT danielatsdepaula synthesiscytotoxicityandantileishmanialactivityofnndisubstitutedethylenediamineandimidazolidinederivatives AT elainescoimbra synthesiscytotoxicityandantileishmanialactivityofnndisubstitutedethylenediamineandimidazolidinederivatives AT adilsonddasilva synthesiscytotoxicityandantileishmanialactivityofnndisubstitutedethylenediamineandimidazolidinederivatives |