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

• Published in: Bioorganic & medicinal chemistry Vol. 11; no. 23; pp. 5013 - 5023
• Main Authors: FAKHFAKH, Mohammed A, FOURNET, Alain, PRINA, Eric, MOUSCADET, Jean-Francois, FRANCK, Xavier, HOCQUEMILLER, Reynald, FIGADERE, Bruno
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Science 17.11.2003
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Antiviral agents; Biological and medical sciences; Drug Evaluation, Preclinical; Female; HIV Infections - complications; HIV Infections - drug therapy; HIV-1 - drug effects; Humans; Leishmania - classification; Leishmania - drug effects; Medical sciences; Mice; Mice, Inbred BALB C; Pharmacology. Drug treatments; 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; Kinetoplastida; Protozoa; HIV-1 virus; Nitrogen heterocycle; Retroviridae; Quinoline derivatives; Lentivirus; In vitro; Virus; Antiprotozoal agent; Structure activity relation; Leishmania; Bicyclic compound; Parasiticide; Antiviral; Aromatic compound; Human immunodeficiency virus; Chemical synthesis; Amastigote
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/j.bmc.2003.09.007

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.