title: Synthesis and in vitro evaluation of new ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide against Entamoeba histolytica.
abstract: In our search for new antiamoebic agents, a new series of ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives have been synthesized using the Beirut reaction. All compounds were characterized by spectroscopic techniques and elemental analysis. Antiamoebic activity was evaluated in vitro against Entamoeba histolytica strain HM1:IMSS by the microdilution method, and the structure-activity relationship was analyzed. We found that eleven quinoxaline derivatives showed greater activity than metronidazole and nitazoxanide with IC₅₀ values in the range 1.99-0.35 μM. Compounds T-001 and T-016 shows IC₅₀ values of 1.41 and 1.47 μM, respectively, with a value of selectivity index >60.
authors.affiliation: Laboratorio de Microbiología, Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001, 62209 Cuernavaca, Mexico.
authors.forename: Blanca Estela
authors.initials: BE
authors.lastname: Duque-Montaño
authors.forename: Lilia Citlalli
authors.initials: LC
authors.lastname: Gómez-Caro
authors.forename: Mario
authors.initials: M
authors.lastname: Sanchez-Sanchez
authors.forename: Antonio
authors.initials: A
authors.lastname: Monge
authors.forename: Efrén
authors.initials: E
authors.lastname: Hernández-Baltazar
authors.forename: Gildardo
authors.initials: G
authors.lastname: Rivera
authors.forename: Oscar
authors.initials: O
authors.lastname: Torres-Angeles
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003497:Cyclic N-Oxides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004748:Entamoeba histolytica / Q000187:drug effects*; D008958:Models, Molecular; D015394:Molecular Structure; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D003497:Cyclic N-Oxides; D011810:Quinoxalines