title: New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities.
abstract: Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, 14 new 3-amino-1,4-di-N-oxide quinoxaline-2-carbonitrile derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum Colombian FCR-3 strain and Leishmania amazonensis strain MHOM/BR/76/LTB-012A. Further computational studies were carried out in order to analyze graphic SAR and ADME properties. The results obtained indicate that compounds with one halogenous group substituted in position 6 and 7 provide an efficient approach for further development of antimalarial and antileishmanial agents. In addition, interesting ADME properties were found.
authors: Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, Pamplona, Spain.
authors: Carlos
authors: C
authors: Barea
authors: Adriana
authors: A
authors: Pabón
authors: Denis
authors: D
authors: Castillo
authors: Mirko
authors: M
authors: Zimic
authors: Miguel
authors: M
authors: Quiliano
authors: Silvia
authors: S
authors: Galiano
authors: Silvia
authors: S
authors: Pérez-Silanes
authors: Antonio
authors: A
authors: Monge
authors: Eric
authors: E
authors: Deharo
authors: Ignacio
authors: I
authors: Aldana
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D007894:Leishmania mexicana / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects / Q000276:immunology; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects; D011810:Quinoxalines / Q000737:chemistry*; D012457:Salicylamides / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity
chemical_list: D000962:Antimalarials; D011810:Quinoxalines; D012457:Salicylamides; D013449:Sulfonamides; D014344:Trypanocidal Agents; C031060:salicylamide