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

Autor(es)

Mizuno, Cassia S. ^[1] ; Souza, Ariana B. ^[2] ; Tekwani, Babu L. ^[3] ; Ambrosio, Sergio R. ^[2] ; Veneziani, Rodrigo C. S. ^[2]

Afiliação do(s) autor(es)

^[1] Univ New England, Coll Pharm, Dept Pharmaceut Sci, Portland, ME 04103 - USA

^[2] Univ Franca, Nucleo Pesquisa Ciencias Exatas & Tecnol, BR-14404600 Franca, SP - Brazil

^[3] Univ Mississippi, Sch Pharm, Natl Ctr Nat Prod Res, University, MS 38677 - USA

• Tipo de documento: Artigo Científico
• Fonte: Bioorganic & Medicinal Chemistry Letters; v. 25, n. 23, p. 5529-5531, DEC 1 2015.
• Citações Web of Science: 5

Resumo

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 mu g/mL. The compound with best antileishmanial activity was 2h (IC50 = 3.84 mu g/mL) and compound 2c showed the best antitrypanosomal activity with an IC50 of 2.54 mu g/mL. (C) 2015 Elsevier Ltd. All rights reserved. (AU)

• Processo FAPESP: 11/13630-7 - Validação química e farmacológica de extratos e princípios ativos de espécies de Copaifera
• Beneficiário: Jairo Kenupp Bastos
• Modalidade de apoio: Auxílio à Pesquisa - Temático
• Processo FAPESP: 11/23493-7 - Óleo-resina de duas espécies de Copaifera: isolamento de metabólitos secundários e desenvolvimento e validação de metodologia analítica por CLAE
• Beneficiário: Ariana Borges Souza
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto