A minimalistic approach to develop new anti-apicomplexa polyamines analogs.

Authors

• Esteban Panozzo-Zénere, Instituto de Química Rosario (IQUIR-CONICET)
• Exequiel O. J. Porta, Instituto de Química Rosario (IQUIR-CONICET)
• Gustavo Arrizabalaga, Indiana University
• Lucía Fargnoli, Instituto de Química Rosario (IQUIR-CONICET)
• Shabana I. Khan, University of Mississippi
• Babu L. Tekwani, University of Mississippi
• Guillermo R. Labadie, Instituto de Química Rosario (IQUIR-CONICET)

Department

Pharmacy

Document Type

Article

DOI

10.1016/j.ejmech.2017.11.069

Publication Date

1-1-2018

Abstract

The development of new chemical entities against the major diseases caused by parasites is highly desired. A library of thirty diamines analogs following a minimalist approach and supported by chemoinformatics tools have been prepared and evaluated against apicomplexan parasites. Different member of the series of N,N'-disubstituted aliphatic diamines shown in vitro activities at submicromolar concentrations and high levels of selectivity against Toxoplasma gondii and in chloroquine-sensitive and resistant-strains of Plasmodium falciparum. In order to demonstrate the importance of the secondary amines, ten N,N,N',N'-tetrasubstituted aliphatic diamines derivatives were synthesized being considerably less active than their disubstituted counterpart. Theoretical studies were performed to establish the electronic factors that govern the activity of the compounds.

Relational Format

journal article

Recommended Citation

Panozzo-Zénere, E. A., Porta, E. O. J., Arrizabalaga, G., Fargnoli, L., Khan, S. I., Tekwani, B. L., & Labadie, G. R. (2018). A minimalistic approach to develop new anti-apicomplexa polyamines analogs. European Journal of Medicinal Chemistry, 143, 866–880. https://doi.org/10.1016/j.ejmech.2017.11.069

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