title: Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles.
abstract: The influence of various structural patterns in a series of novel bi- and tricyclic N-heterocycles on the activity against Leishmania major and Leishmania panamensis has been studied and compounds that are active in the low micromolar region have been identified. Both quinolines and tetrahydrooxazinoindoles (TOI) proved to have significant antileishmanial activities, while substituted indoles were inactive. We have also showed that a chloroquine analogue induces Leishmania killing by modulating macrophage activation.
authors.affiliation: Centro de Biología Molecular y Celular de Enfermedades, Instituto de Investigaciones Científicas y de Alta Tecnología (INDICASAT-AIP), Edificio 219, Ciudad del Saber, Apartado 0843-01103, Panamá, República de Panamá. pllanes@indicasat.org.pa.
authors.forename: Lizzi
authors.initials: L
authors.lastname: Herrera
authors.forename: David E
authors.initials: DE
authors.lastname: Stephens
authors.forename: Abigail
authors.initials: A
authors.lastname: D'Avila
authors.forename: Kathryn G
authors.initials: KG
authors.lastname: George
authors.forename: Hadi
authors.initials: H
authors.lastname: Arman
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhang
authors.forename: George
authors.initials: G
authors.lastname: Perry
authors.forename: Ricardo
authors.initials: R
authors.lastname: Lleonart
authors.forename: Oleg V
authors.initials: OV
authors.lastname: Larionov
authors.forename: Patricia L
authors.initials: PL
authors.lastname: Fernández
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D016753:Interleukin-10 / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D007891:Leishmania / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D006571:Heterocyclic Compounds; D016753:Interleukin-10