Synthesis and evaluation of activity of gibbilimbol B derivatives in Trypanosoma cruzi

• Grant number: 14/16564-3
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: January 01, 2015
• End date: December 31, 2015
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: João Paulo dos Santos Fernandes
• Grantee: Marina Themoteo Varela
• Host Institution: Instituto de Ciências Ambientais, Químicas e Farmacêuticas (ICAQF). Universidade Federal de São Paulo (UNIFESP). Campus Diadema. Diadema , SP, Brazil

Abstract

American trypanosomiasis, commonly known as Chagas' disease, is one of the three most important pathologies caused by protozoa considered as neglected diseases. Caused by the infection of Trypanossoma cruzi, an obligatory intracellular parasite transmitted mainly by Triatoma infestans, intermediate host, holds responsibility for the death of nearly 14,000 people every year in Latin America. The disease is currently treated by two available drugs, benznidazole and nifurtimox, whose efficacy is only significant during the acute phase, which is not often diagnosed in time. A natural product, gibbilimbol B, showed promising activity against parasite strains, 10-fold higher than benznidazole. In order to search for new options of treatment, the present project uses gibbilimbol B as a prototype for the development new molecules with potential trypanocidal activity. The suggested molecules aim to exploring structural features that determine the activity of gibbilimbol B and to help further design of new chemical entities with better activity and lower toxicity. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

VARELA, MARINA T.; DIAS, ROBERTO Z.; MARTINS, LIGIA F.; FERREIRA, DAIANE D.; TEMPONE, ANDRE G.; UENO, ANDERSON K.; LAGO, JOAO HENRIQUE G.; FERNANDES, JOAO PAULO S.. Gibbilimbol analogues as antiparasitic agents-Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum. Bioorganic & Medicinal Chemistry Letters, v. 26, n. 4, p. 1180-1183, FEB 15 2016. (13/20479-9, 12/18756-1, 15/11936-2, 14/16564-3)

CORREA, MICHELLE FIDELIS; VARELA, MARINA THEMOTEO; BALBINO, ALEKSANDRO MARTINS; TORRECILHAS, ANA CLAUDIA; LANDGRAF, RICHARDT GAMA; PAOLO TRONCONE, LANFRANCO RANIERI; DOS SANTOS FERNANDES, JOAO PAULO. 1-[(2,3-Dihydro-1-benzofuran-2-yl) methyl]piperazines as novel anti-inflammatory compounds: Synthesis and evaluation on H3R/H4R. CHEMICAL BIOLOGY & DRUG DESIGN, v. 90, n. 2, p. 317-322, AUG 2017. (13/20479-9, 13/18897-7, 14/16564-3)