Banca de QUALIFICAÇÃO: PAULO PITASSE SANTOS

Uma banca de QUALIFICAÇÃO de DOUTORADO foi cadastrada pelo programa.
DISCENTE : PAULO PITASSE SANTOS
DATA : 23/01/2018
HORA: 10:00
LOCAL: ICE- PPGQ - Sala 50
TÍTULO:

Planning and Synthesis of 1,2,4- and 1,3,4-oxadiazolic Derivatives as

Potential Inhibitors of RdRp-NS5 Dengue Virus .

PALAVRAS-CHAVES:

oxadiazoles, dengue, antiviral, NS5-RdRp inhibitors 

PÁGINAS: 20
GRANDE ÁREA: Ciências Exatas e da Terra
ÁREA: Química
RESUMO:

Dengue is a disease that occurs in at least 128 countries, and accounts for 50 million new cases annually. Its etiological agent is the dengue virus, which presents in four serotypes. It is transmitted through the bite of mosquitoes of the genus Aedes, especially Aedes aegypti. The investigation of the mechanism of action of the virus in the host organism have identified the viral non-structural enzyme RNA polymerase (NS5-RdRp) as a promising therapeutic target. This project presents a series of analogues to the 3-aryl-4-methoxy-benzylic acid NS5-RdRp inhibitors. The molecular planning of candidates is based on the maintenance of the pharmacophore group 4-methoxy-benzylic acid and the substitution of the 3-aryl group by the 1,2,4- and 1,3,4-oxadiazole heterocycles. In addition substituent groups with lipophilic profile are to be included at position 5 of the heterocyclic rings. It is thus intended to explore the presence of a lipophilic pocket at the back of the active site of NS5-RdRp. The proposed synthetic methodology involves 5 reactional steps to furnish each of the series of 1,2,4- and 1,3,4-oxadiazolic heterocyclic derivatives. The use of common reagents and reaction steps to both synthetic routes simplifies the experimental procedure for obtaining the derivatives. The in vitro assessment to verify the inhibitory activity against RdRp-NS5 of the compounds synthesized will be carried out in collaboration with the Crystallography Group of the University of São Paulo in São Carlos-SP (IFSC / USP), under the supervision of Prof. Glaucius Oliva.

MEMBROS DA BANCA:
Presidente - 387189 - AUREA ECHEVARRIA AZNAR NEVES LIMA
Externo ao Programa - 1808299 - DEBORA REGINA LOPES DOS SANTOS
Interno - 1221906 - LUCIANO RAMOS SUZART