Antiparasitary potential evaluation for a group of labdane diterpenes against Leishmania amazonensis

• Grant number: 13/21167-0
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: December 01, 2013
• End date: December 31, 2014
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Vladimir Constantino Gomes Heleno
• Grantee: Priscilla Mendonça Matos
• Host Institution: Pró-Reitoria Adjunta de Pesquisa e Pós-Graduação. Universidade de Franca (UNIFRAN). Franca , SP, Brazil
• Associated research grant: 11/13630-7 - Chemical and pharmacological validation of extracts and active compounds of Copaifera species, AP.TEM
• Associated scholarship(s): 14/06971-0 - Obtaining new derivatives of copalic acid: and evaluation of their biological activities, BE.EP.IC

Abstract

This proposal involves the structural modification of natural diterpenes by semi-synthetic methods in the search for active compounds against the leishmaniasis parasite Leishmania amazonensis. Those natural diterpenes will be isolated from a commercial source of copaiba oil already obtained. After isolation, copalic acid and ent-agatic acid will be submitted to three reactions each. Those reactions were studied by the proponent student with a different substract in her foreign internship through "Ciência sem Fronteiras"-CNPq. In the ocasion, the student got in touch with those reactions and, now, we will perform them with different diterpenes. We expect to reach at least six derivatives for our biological activities assays. They will be evaluated regarding their antiparasitary potential against promastigote forms of L. amazonensis.This project is linked to a Thematical Project (2011/13630-7), which it may support by providing derivatives for the proposed biological assays. Our experience enables the use of other isolated structures to get even more derivatives if there is time for it. Furthermore, we can submitt the acid diterpenes obtained to sterification reactions and significantly rise the total number of derivatives - maybe to 20.Structural determination will be held by NMR, by the use of 1H-NMR, 13C-NMR, COSY, HSQC, HMBC, DPFGSE-NOE and J-resolved experiments as necessary.