title: Synthesis of new quinazolin-2,4-diones as anti-Leishmania mexicana agents.
abstract: The quinazolin-2,4-dione moiety is found in many compounds with important biological activities making it a target for its synthesis. In this work, a one-pot three-step synthesis of new quinazolin-2,4-diones from phthalic anhydrides and their activity against Leishmania mexicana are described. The new quinazolin-2,4-diones were isolated with yields in the range of 32-70 %. All compounds displayed lower cytotoxicity in RAW 264.7 macrophage over miltefosine. Compound 6,7-dichloro-3-phenylquinazoline-2,4(1H,3H)-dione (6e) displayed an attractive profile which includes anti-Leishmania mexicana activity ([Formula: see text] [Formula: see text]M), much lower cytotoxic activity ([Formula: see text] [Formula: see text]M) and a high selective index ([Formula: see text]) proving to be superior to miltefosine.
authors.affiliation: Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Sinaloa, Blvd. de las Ámericas S/N, C.P. 80040, Culiacán Rosales, Sinaloa, Mexico.
authors.forename: Eduardo
authors.initials: E
authors.lastname: Enciso
authors.affiliation: Facultad de Ingeniería Culiacán, Universidad Autónoma de Sinaloa, Blvd. de las Ámericas S/N, C.P. 80040, Culiacán Rosales, Sinaloa, Mexico. jsarmiento@uas.edu.mx.
authors.forename: Juan I
authors.identifier: http://orcid.org/0000-0001-8961-4436
authors.initials: JI
authors.lastname: Sarmiento-Sánchez
authors.affiliation: Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Sinaloa, Blvd. de las Ámericas S/N, C.P. 80040, Culiacán Rosales, Sinaloa, Mexico.
authors.forename: Héctor S
authors.initials: HS
authors.lastname: López-Moreno
authors.affiliation: Centro de Graduados e Investigación en Química, Instituto Tecnológico de Tijuana, Blvd. Alberto Limón Padilla S/N, Mesa de Otay, 22500, Tijuana, B.C., Mexico.
authors.forename: Adrián
authors.initials: A
authors.lastname: Ochoa-Terán
authors.affiliation: Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Sinaloa, Blvd. de las Ámericas S/N, C.P. 80040, Culiacán Rosales, Sinaloa, Mexico.
authors.forename: Ulises
authors.initials: U
authors.lastname: Osuna-Martínez
authors.affiliation: Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Sinaloa, Blvd. de las Ámericas S/N, C.P. 80040, Culiacán Rosales, Sinaloa, Mexico.
authors.forename: Evangelina
authors.initials: E
authors.lastname: Beltrán-López
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D020128:Inhibitory Concentration 50; D007894:Leishmania mexicana / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000494:pharmacology; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D052999:Quinazolinones; D010767:Phosphorylcholine; C039128:miltefosine
keywords: Leishmania mexicana; Phthalic anhydrides; Quinazolin-2,4-dione; RAW 264.7 macrophage