Synthesis and biological evaluation of polyalthic acid derivatives for the treatment of neglected diseases.

Autor: Mizuno CS; Department of Pharmaceutical Sciences, University of New England College of Pharmacy, 716 Stevens Ave, Portland, ME 04103, USA. Electronic address: cmizuno@une.edu., Souza AB; 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., Tekwani BL; National Center for Natural Products Research, School of Pharmacy, University of Mississippi, MS 38677, USA., Ambrósio SR; 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., Veneziani RC; 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.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Dec 01; Vol. 25 (23), pp. 5529-31. Date of Electronic Publication: 2015 Oct 21.
DOI: 10.1016/j.bmcl.2015.10.062
Abstrakt: 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.
(Copyright © 2015 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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