title: Synthesis and biological evaluation of polyalthic acid derivatives for the treatment of neglected diseases.
abstract: Polyalthic acid is a naturally occurring diterpene found in copaiba oil, one of the most popular natural medicines in the Amazon. Based on the reported antileishmanial activity of copaiba oil, a series of amides and diols derivatives of polyalthic acid were synthesized and tested against Leishmania donovani and Trypanosoma brucei. Polyalthic acid was active in both assays with IC50 ranging from 3.87 to 8.68 μg/mL. The compound with best antileishmanial activity was 2 h (IC50=3.84 μg/mL) and compound 2c showed the best antitrypanosomal activity with an IC50 of 2.54 μg/mL.
authors.affiliation: Department of Pharmaceutical Sciences, University of New England College of Pharmacy, 716 Stevens Ave, Portland, ME 04103, USA. Electronic address: cmizuno@une.edu.
authors.forename: Cassia S
authors.initials: CS
authors.lastname: Mizuno
authors.affiliation: Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, 14404-600 Franca, SP, Brazil.
authors.forename: Ariana B
authors.initials: AB
authors.lastname: Souza
authors.affiliation: National Center for Natural Products Research, School of Pharmacy, University of Mississippi, MS 38677, USA.
authors.forename: Babu L
authors.initials: BL
authors.lastname: Tekwani
authors.affiliation: Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, 14404-600 Franca, SP, Brazil.
authors.forename: Sérgio R
authors.initials: SR
authors.lastname: Ambrósio
authors.affiliation: Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, 14404-600 Franca, SP, Brazil. Electronic address: rcsvenez@gmail.com.
authors.forename: Rodrigo C S
authors.initials: RC
authors.lastname: Veneziani
mesh_terms: D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D015394:Molecular Structure; D058069:Neglected Diseases / Q000188:drug therapy; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D000977:Antiparasitic Agents; D004224:Diterpenes; D014344:Trypanocidal Agents; C000611189:polyalthic acid
keywords: Copaiba oil; Leishmaniasis; Polyalthic acid; Trypanosomiasis