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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
VOLUME: 9
ISSUE: 8
DOI: 10.2174/157018012802652994      Price:  $58









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

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Author(s): Arnold R. Romero Bohorquez, Patricia Escobar Rivero, Sandra M. Leal and Vladimir V. Kouznetsov
Pages 802-808 (7)
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).
Keywords:
Antiparasitic activities, Cytotoxicity, Imino Diels-Alder reaction, Leishmania chagasi, Tetrahydroquinolines, Trypanosoma cruzi, paromomycin, Leishmania and Trypanosoma, flagellated protozoa, anti-leishmanial
Affiliation:
Laboratorio de Quimica Organica y Biomolecular, Escuela de Quimica, Universidad Industrial de Santander, A.A. 678, Bucaramanga, Colombia.