title: Synthesis and in vitro trypanocide activity of several polycyclic drimane-quinone derivatives.
abstract: The Diels-Alder reaction between two polygodial-derived dienes and simple quinones to yield substituted naphtho- and anthraquinones, is described. The in vitro trypanocide activity for the series was determined. Two of the new compounds showed an activity ten and two times higher, respectively, than nifurtimox and benznidazole, the medicines of choice for the treatment of the acute Chagas' disease.
authors.affiliation: Departamento de Química Orgánica, Facultad de Química, Pontificia Universidad Católica de Chile, Vicuña Mackenna 4860, Casilla 306, Correo 22, Santiago, Chile.
authors.forename: Mauricio A
authors.initials: MA
authors.lastname: Cuellar
authors.forename: Cristian
authors.initials: C
authors.lastname: Salas
authors.forename: Manuel J
authors.initials: MJ
authors.lastname: Cortés
authors.forename: Antonio
authors.initials: A
authors.lastname: Morello
authors.forename: Juan
authors.initials: J
authors.lastname: Diego Maya
authors.forename: Marcelo D
authors.initials: MD
authors.lastname: Preite
mesh_terms: D000818:Animals; D020128:Inhibitory Concentration 50; D009547:Nifurtimox / Q000494:pharmacology; D009593:Nitroimidazoles / Q000494:pharmacology; D011083:Polycyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D000081223:Polycyclic Sesquiterpenes; D011809:Quinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects / Q000254:growth & development
chemical_list: D009593:Nitroimidazoles; D011083:Polycyclic Compounds; D000081223:Polycyclic Sesquiterpenes; D011809:Quinones; D012717:Sesquiterpenes; D014344:Trypanocidal Agents; C437376:drimane; D009547:Nifurtimox; C009999:benzonidazole