IQUIR   05412
INSTITUTO DE QUIMICA ROSARIO
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
Substituted diamines with potent antiparasitic activity
Autor/es:
LABADIE, GUILLERMO R.; CAMINOS, ANDREA P.; PANOZZO, ESTEBAN A.; TEKWANI, BABU
Lugar:
Breckenridge, CO, USA
Reunión:
Simposio; Keystone Symposia: Drug Discovery for Protozoan Parasites (D2); 2009
Institución organizadora:
Keystone Symposia on molecular and cellular biology
Resumen:
Polyamines are essential for cellular differentiation and proliferation. It has been shown those metabolites transport and biosynthesis are a valid target for drug discovery and development toward parasitic diseases.In our search of new chemotherapies against parasitic diseases we wanted to interfere on process were those metabolites are involved. To do that, we have prepared a different libraries of N,N,N’,N’–tetrasubstituted, N,N´- and N,N-disubtituted diamines, using solution or solid phase synthesis. The libraries prepared were tested against the parasite responsible of the visceral leishmaniasis (L. donovani) and two different strain of P. falciparum, (Chloroquine sensitive and resistant) looking for antimalarial activity. In general, the N,N´-disubtituted diamines have the best profile against both diseases with submicromolar IC50 as antimalarial and nanomolar as antileishmanial. Structural activity profile of the libraries prepared will be discussed as long as the future directions of the project.