Antiinfective compounds: bringing together medicinal chemistry and organic synthesis in search of lead antiparasitic compounds

• Grant number: 09/14184-0
• Support Opportunities: Regular Research Grants
• Start date: December 01, 2009
• End date: November 30, 2011
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Flavio da Silva Emery
• Grantee: Flavio da Silva Emery
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Infectious diseases account for a large number of hospitalizations and death in hospitals in the National Health System (SUS), generating a cost of more than 500 million reais last year. Among the most important diseases are leishmaniasis, malaria and AIDS, in which the therapies are costly or ineffective or even toxic. Therefore, this project aims to study the design and synthesis of new agents capable of acting on the parasitic diseases Malaria and Leishmaniasis, in order to obtain innovative prototypes through medicinal chemistry methods, such as molecular hybridization and bioisosterismo, besides organic synthesis, as well as collaborations with research groups involved in biological assays, featuring a multidisciplinary project able of forming qualified human resources in drug discovery approaches. (AU)

Scientific publications

(9)

(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)

CASTRO, FELIPE FREITAS; RUY, PATRICIA C.; ZEVIANI, KARMA NOGUEIRA; SANTOS, RAMON FREITAS; TOLEDO, JULIANO SIMOES; CRUZ, ANGELA KAYSEL. Evidence of putative non-coding RNAs from Leishmania untranslated regions. Molecular and Biochemical Parasitology, v. 214, p. 69-74, JUN 2017. (13/50219-9, 12/16749-8, 09/14184-0, 12/17025-3)

VESSECCHI, RICARDO; EMERY, FLAVIO S.; GALEMBECK, SERGIO E.; LOPES, NORBERTO P.. Fragmentation studies and electrospray ionization mass spectrometry of lapachol: protonated, deprotonated and cationized species. RAPID COMMUNICATIONS IN MASS SPECTROMETRY, v. 24, n. 14, p. 2101-2108, JUL 2010. (05/01572-1, 09/08281-3, 09/14184-0)

DE TOLEDO, JULIANO S.; JUNIOR, PAULO E. S.; MANFRIM, VIVIANE; PINZAN, CAMILA F.; DE ARAUJO, ALEXANDRE S.; CRUZ, ANGELA K.; EMERY, FLAVIO S.. Synthesis, Cytotoxicity and In Vitro Antileishmanial Activity of Naphthothiazoles. CHEMICAL BIOLOGY & DRUG DESIGN, v. 81, n. 6, p. 749-756, JUN 2013. (09/51812-0, 09/14184-0)

DIAS DE REZENDE, LUCAS CUNHA; FUMAGALLI, FERNANDO; BORTOLIN, MARRAIANA SCHIAVON; DE OLIVEIRA, MARIANNE GARCIA; DE PAULA, MURILO HELDER; DE ANDRADE-NETO, VALTER FERREIRA; EMERY, FLAVIO DA SILVA. In vivo antimalarial activity of novel 2-hydroxy-3-anilino-1,4-naphthoquinones obtained by epoxide ring-opening reaction. Bioorganic & Medicinal Chemistry Letters, v. 23, n. 16, p. 4583-4586, AUG 15 2013. (09/14184-0)

PINHEIRO, MATHEUS PINTO; EMERY, FLAVIO DA SILVA; CRISTINA NONATO, M.. Target Sites for the Design of Anti-trypanosomatid Drugs Based on the Structure of Dihydroorotate Dehydrogenase. CURRENT PHARMACEUTICAL DESIGN, v. 19, n. 14, p. 2615-2627, APR 2013. (09/14184-0, 07/08703-0)

SANTOS, GABRIELA B.; KROGH, RENATA; MAGALHAES, LUMA G.; ANDRICOPULO, ADRIANO D.; PUPO, MONICA T.; EMERY, FLAVIO S.. Semisynthesis of new aphidicolin derivatives with high activity against Trypanosoma cruzi. Bioorganic & Medicinal Chemistry Letters, v. 26, n. 4, p. 1205-1208, FEB 15 2016. (13/07600-3, 09/14184-0)

SANTOS, GABRIELA B.; ALMEIDA, MARILIA O.; CARDOSO, IARA A.; MANFRIM, VIVIANE; CHAGAS, FERNANDA O.; TOLEDO, JULIANO S.; PINZAN, CAMILA C.; DE ARAUJO, ALEXANDRE SUMAN; CRUZ, ANGELA K.; PUPO, MONICA T.; et al. The semisynthetic landscape of aphidicolin: inspiration towards leishmanicidal compounds. Journal of the Brazilian Chemical Society, v. 25, n. 10, p. 1885+, OCT 2014. (09/51812-0, 09/14184-0)

ANDRADE, MICASSIO F.; KABEYA, LUCIANA M.; AZZOLINI, ANA ELISA C. S.; SANTOS, EVERTON O. L.; FIGUEIREDO-RINHEL, ANDREA S. G.; PARIS, MARCIO R. P.; EMERY, FLAVIO S.; PUPO, MONICA T.; LUCISANO-VALIM, YARA M.. 3-Phenylcoumarin derivatives selectively modulate different steps of reactive oxygen species production by immune complex-stimulated human neutrophils. International Immunopharmacology, v. 15, n. 2, p. 387-394, FEB 2013. (09/14184-0, 07/02487-3, 07/00840-8)

DA SILVA JUNIOR, EUFRANIO N.; DE MELO, ISADORA M. M.; DIOGO, EMILAY B. T.; COSTA, VERENICE A.; DE SOUZA FILHO, JOSE D.; VALENCA, WAGNER O.; CAMARA, CELSO A.; DE OLIVEIRA, RONALDO N.; DE ARAUJO, ALEXANDRE S.; EMERY, FLAVIO S.; et al. On the search for potential anti-Trypanosoma cruzi drugs: Synthesis and biological evaluation of 2-hydroxy-3-methylamino and 1,2,3-triazolic naphthoquinoidal compounds obtained by click chemistry reactions. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 52, p. 304-312, JUN 2012. (09/51812-0, 09/14184-0)