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

Author(s)

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

Affiliation

^[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

• Document type: Journal article
• Source: Bioorganic & Medicinal Chemistry Letters; v. 25, n. 23, p. 5529-5531, DEC 1 2015.
• Web of Science Citations: 5

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 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)

• FAPESP's process: 11/13630-7 - Chemical and pharmacological validation of extracts and active compounds of Copaifera species
• Grantee: Jairo Kenupp Bastos
• Support Opportunities: Research Projects - Thematic Grants
• FAPESP's process: 11/23493-7 - Two Copaifera species oleoresin: secondary metabolites isolation and development and validation of HPLC analytical methodology
• Grantee: Ariana Borges Souza
• Support Opportunities: Scholarships in Brazil - Doctorate (Direct)