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Sci. Pharm. 2013, 81(1), 43-56; doi:10.3797/scipharm.1205-14

In Vitro Antileishmanial, Trypanocidal, and Mammalian Cell Activities of Diverse N,N'-Dihetaryl Substituted Diamines and Related Compounds

1
Centro de Investigación de Enfermedades Tropicales, CINTROP, Departamento de Ciencias Básicas, Escuela de Medicina, Universidad Industrial de Santander, Bucaramanga, Colombia
2
Laboratorio de Química Orgánica y Biomolecular, Escuela de Química, Universidad Industrial de Santander, Bucaramanga, Colombia
*
Author to whom correspondence should be addressed.
Received: 31 May 2012 / Accepted: 14 October 2012 / Published: 14 October 2012
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Abstract

The leishmaniasis and Chagas diseases constitute a serious public health problem worldwide with few and ineffective treatment options. The search for new antiparasitic candidates at the initial steps of drug discovery and development is still necessary. The synthesis of 22 de novo synthetized N,N'-dihetaryl-alkyldiamine derivatives and in vitro antiparasitic activity were evaluated for the first time against intracellular and extracellular forms of Leishmania (Leishmania) infantum, L. (Viannia) panamensis, L. (Leishmania) amazonensis, and Trypanosoma cruzi. Additionally, the toxicity on mammalian cells was determined. Some of these substituted N,N'-diamines (25–35 % of the tested compounds) showed interesting results against free-living forms of parasites with activities at the inhibitory concentration (IC50) level of 1.96 to 28.83 μM for L. (L.) infantum promastigotes and IC50 of 0.02 to 5.31 μM for T. cruzi epimastigotes. No activity at the IC50 level on intracellular amastigotes of T. cruzi was observed. However, N1,N2-dibenzylethane-1,2-diamine 5a revealed an important activity against the intracellular amastigotes of L. infantum (IC50 25.42 μM ±0.33) and L. panamensis (IC50 58.20 μM ±3.23), while their analogue N1,N4-dibenzylbutane-1,4-diamine 5c resulted in activity only against L. panamensis (IC50 11.19 μM ±0.20) without toxicity on Vero and THP-1 mammalian cells. The active compounds against intracellular parasites with low toxicity in mammalian cells may be considered for future studies in experimental models.
Keywords: Leishmania (Leishmania) infantum; Leishmania (Viannia) panamensis; Trypanosoma cruzi; Mammalian cell toxicity; N,N'-Dihetaryl-alkyldiamine derivatives; Drug discovery Leishmania (Leishmania) infantum; Leishmania (Viannia) panamensis; Trypanosoma cruzi; Mammalian cell toxicity; N,N'-Dihetaryl-alkyldiamine derivatives; Drug discovery
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

LEAL, S.M.; AMADO, D.F.; KOUZNETSOV, V.V.; ESCOBAR, P. In Vitro Antileishmanial, Trypanocidal, and Mammalian Cell Activities of Diverse N,N'-Dihetaryl Substituted Diamines and Related Compounds. Sci. Pharm. 2013, 81, 43-56.

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