In Vitro Activity Against Trypanosoma cruzi and Leishmania chagasi Parasites of 2,4-Diaryl 1,2,3,4-Tetrahydroquinoline Derivatives

Title:In Vitro Activity Against Trypanosoma cruzi and Leishmania chagasi Parasites of 2,4-Diaryl 1,2,3,4-Tetrahydroquinoline Derivatives

Volume: 9 Issue: 8

Author(s): Arnold R. Romero Bohorquez, Patricia Escobar Rivero, Sandra M. Leal and Vladimir V. Kouznetsov

Affiliation:

Keywords: Antiparasitic activities, Cytotoxicity, Imino Diels-Alder reaction, Leishmania chagasi, Tetrahydroquinolines, Trypanosoma cruzi, paromomycin, Leishmania and Trypanosoma, flagellated protozoa, anti-leishmanial

Abstract: Diverse polyfunctionalized tetrahydroquinolines, easily prepared using BF3 .OEt2-catalyzed three component imino Diels–Alder reaction, were tested in vitro against Trypanosoma cruzi and Leishmania chagasi parasites and also for cytotoxicity using Vero and THP-1 mammalian cell lines. These studies showed that the most active compound was 7h (IC50 5.77 ± 0.21; IC90 40.43 ± 1.58 μM for T. cruzi and IC50 0.27 ± 0.03; IC90 2.16± 0.37 μM for L. chagasi) has selective index (SI) values greater than the reference drugs (SI > 46 and SI > 1000 in epimastigotes form of T. cruzi and promastigotes form of L. chagasi parasites, respectively). Moreover, the comp. 7h did not show cytotoxicity against Vero or THP-1 cells (IC50 > 270 μM).

Cite this article as:

R. Romero Bohorquez Arnold, Escobar Rivero Patricia, M. Leal Sandra and V. Kouznetsov Vladimir, In Vitro Activity Against Trypanosoma cruzi and Leishmania chagasi Parasites of 2,4-Diaryl 1,2,3,4-Tetrahydroquinoline Derivatives, Letters in Drug Design & Discovery 2012; 9 (8) . https://dx.doi.org/10.2174/157018012802652994