Synthesis and biological evaluation of substituted quinolines: potential treatment of protozoal and retroviral co-infections

Mohammed A Fakhfakh; Alain Fournet; Eric Prina; Jean-François Mouscadet; Xavier Franck; Reynald Hocquemiller; Bruno Figadère

doi:10.1016/j.bmc.2003.09.007

Synthesis and biological evaluation of substituted quinolines: potential treatment of protozoal and retroviral co-infections

Bioorg Med Chem. 2003 Nov 17;11(23):5013-23. doi: 10.1016/j.bmc.2003.09.007.

Authors

Mohammed A Fakhfakh¹, Alain Fournet, Eric Prina, Jean-François Mouscadet, Xavier Franck, Reynald Hocquemiller, Bruno Figadère

Affiliation

¹ Laboratoire de Pharmacognosie (associé au CNRS-BioCIS), Faculté de Pharmacie, Université Paris-Sud, rue J.B. Clément, 92296, Châtenay-Malabry, France.

PMID: 14604664
DOI: 10.1016/j.bmc.2003.09.007

Abstract

We report the synthesis of substituted quinolines and their in vitro biological evaluation against the causal agents of cutaneous leishmaniasis, visceral leishmaniasis, African trypanosomiasis and Chagas' disease. Furthermore, several quinolines have also been tested for their anti-retroviral activity in HIV-1 infected cells. The structure-activity relationships of these new synthetic compounds are discussed and emphasis was placed on the treatment of leishmania/HIV co-infections.

MeSH terms

Animals
Drug Evaluation, Preclinical
Female
HIV Infections / complications
HIV Infections / drug therapy*
HIV-1 / drug effects
Humans
Leishmania / classification
Leishmania / drug effects
Mice
Mice, Inbred BALB C
Protozoan Infections / complications
Protozoan Infections / drug therapy*
Quinolines / chemical synthesis*
Quinolines / chemistry
Quinolines / pharmacology*
Quinolines / therapeutic use
Structure-Activity Relationship
Trypanosoma / classification
Trypanosoma / drug effects

Substances

Quinolines