Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 4; pp. 815 - 820
• Main Authors: Hui, Xu, Desrivot, Julie, Bories, Christian, Loiseau, Philippe M., Franck, Xavier, Hocquemiller, Reynald, Figadère, Bruno
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15.02.2006; Elsevier
• Subjects: Amides; Amines; Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Antiprotozoal Agents - chemical synthesis; Antiprotozoal Agents - chemistry; Antiprotozoal Agents - pharmacology; Bioassays; Biological and medical sciences; In Vitro Techniques; Leishmania donovani; Leishmania donovani - drug effects; Medical sciences; Molecular Structure; Parasitic Sensitivity Tests; Pharmacology. Drug treatments; Quinoxalines; Quinoxalines - chemical synthesis; Quinoxalines - chemistry; Quinoxalines - pharmacology; Structure-Activity Relationship; Synthesis; Trichomonas vaginalis; Trichomonas vaginalis - drug effects; Trypanosoma brucei brucei; Trypanosoma brucei brucei - drug effects; Quinoxalines; Amides; Amines; Synthesis; Bioassays; Kinetoplastida; Trichomonas vaginalis; Protozoa; Quinoxaline derivatives; Leishmania donovani; Trichomonadida; In vitro; Antiprotozoal agent; Amine; Structure activity relation; Parasiticide; Carboxamide; Chemical synthesis; Trypanosoma brucei
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2005.11.025

A series of substituted quinoxalines (29 compounds) was synthesized and evaluated against several protozoa. Some of them showed promising antileishmanial activity against Leishmania donovani. A series of 29 new quinoxalines was synthesized and evaluated in vitro against several parasites ( Leishmania donovani, Trypanosoma brucei brucei, and Trichomonas vaginalis). Several of them displayed interesting activities, and particularly four quinoxaline amides showed in vitro antileishmanial properties (IC 50 less than 20 μM).