Potential antichagasic agents: design and synthesis of nitric oxide releasing compounds nitrate esters derivatives

• Grant number: 16/03124-0
• Support type: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): June 01, 2016
• Effective date (End): May 31, 2017
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Elizabeth Igne Ferreira
• Grantee: Filipe Gomes Pernichelle
• Home Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Chagas disease is a zoonosis common in Latin America and its transmissions is carried out through the parasite named Trypanosoma cruzi. This is a neglected disease that provokes serious problems for public health in the American continent. However, due to the globalization and illegal immigration of people from the endemic countries, this disease has been disseminated to United States, Canada, Japan and Australia and many European countries as well. Nowadays, there are 21 countries considered endemic with around 100 million people at the risk of the infection, eight million people infected and more than 41 thousand new cases yearly registered. Although this disease had been detected more than a hundred years ago, its chemotherapy still remains scarce, with only two drugs (nifurtimox and benzonidazole) available. Both have low efficacy in the chronic phase of the disease and more than 80% of the patients do not have parasitological cure in this phase. Taking into account this black scenario, it is important to search for more effective compounds against T. cruzi. To face this challenge, and considering the therapy based on nitric oxide (NO) releasing compounds as an interesting approach to design new antiparasitic agents, the purpose of this work is to synthesize eight derivatives of a new series of compounds with hydrazides and nitrate esters as NO releasing groups. (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)

SERAFIM, RICARDO A. M.; PERNICHELLE, FILIPE G.; FERREIRA, ELIZABETH I. The latest advances in the discovery of nitric oxide hybrid drug compounds. EXPERT OPINION ON DRUG DISCOVERY, v. 12, n. 9, p. 941-953, 2017. Web of Science Citations: 8.