title: Antiplasmodial and leishmanicidal activities of 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives.
abstract: Malaria and leishmaniasis are two of the World's most important tropical parasitic diseases. Thirteen new 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives (CPCQs) were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against erythrocytic forms of Plasmodium falciparum and axenic forms of Leishmania infantum. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. None of the tested compounds was efficient against Plasmodium, but two of them showed good activity against Leishmania. Toxicity on VERO was correlated with leishmanicidal properties.
authors.affiliation: Research and Development of Novel Drugs Unit, Center for Applied Pharmacobiology Research-CIFA, University of Navarre, Pamplona 31080, Spain. cabareari@hotmail.com
authors.forename: Carlos
authors.initials: C
authors.lastname: Barea
authors.forename: Adriana
authors.initials: A
authors.lastname: Pabón
authors.forename: Silvia
authors.initials: S
authors.lastname: Galiano
authors.forename: Silvia
authors.initials: S
authors.lastname: Pérez-Silanes
authors.forename: German
authors.initials: G
authors.lastname: Gonzalez
authors.forename: Chloe
authors.initials: C
authors.lastname: Deyssard
authors.forename: Antonio
authors.initials: A
authors.lastname: Monge
authors.forename: Eric
authors.initials: E
authors.lastname: Deharo
authors.forename: Ignacio
authors.initials: I
authors.lastname: Aldana
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002384:Catalysis; D002522:Chlorocebus aethiops; D004126:Dimethylformamide / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D005021:Ethylamines / Q000737:chemistry; D020128:Inhibitory Concentration 50; D018314:Leishmania infantum / Q000187:drug effects*; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*; D011810:Quinoxalines / Q000138:chemical synthesis / Q000494:pharmacology*; D012997:Solvents / Q000737:chemistry; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000981:Antiprotozoal Agents; D005021:Ethylamines; D010879:Piperazines; D011810:Quinoxalines; D012997:Solvents; D004126:Dimethylformamide; C016162:triethylamine