Banca de QUALIFICAÇÃO: RAFAEL FERREIRA DOS SANTOS

Uma banca de QUALIFICAÇÃO de DOUTORADO foi cadastrada pelo programa.
STUDENT : RAFAEL FERREIRA DOS SANTOS
DATE: 06/12/2023
TIME: 13:00
LOCAL: Programa de Pós-graduação em Química
TITLE:

Planning and synthesis of new compounds derived from anacardic acid based on the 1,2,3-triazole heterocycle with potential activity anti-inflammatory.

KEY WORDS:

Cashew Nut, Anacardic acids, anti-inflammatory activity, Cyclo-Oxygenase, 1,2,3-triazole

PAGES: 20
BIG AREA: Ciências Exatas e da Terra
AREA: Química
SUBÁREA: Química Orgânica
SPECIALTY: Química dos Produtos Naturais
SUMMARY:

Cashew nut shell liquid (LCC) is an agro-industrial byproduct that
corresponds to around 25% of the weight of the chestnut. The LCC has characteristics
specific due to its rich composition in alkylphenols such as anacardic acids
(AAs), salicylic acid derivatives; followed by cardols, derived from resorcinol; It is
lower levels of cardanols, derived from anacardic acids. Studies demonstrate
that AAs are capable of inhibiting certain enzymes in the human body, such as
for example, cyclooxygenase (COX-1 and COX-2), COX-1 being constitutively
expressed in human membranes, responsible for renal and platelet homeostasis,
in addition to being highly important in protecting the stomach mucosa; and COX-2,
being expressed inductively to inflammatory stimuli by cytokines and others
mediators at sites of inflammation. Nonsteroidal anti-inflammatory drugs (NSAIDs)
constitute a very heterogeneous group of medicines, being sold in
all over the world with analgesic, antipyretic and anti-inflammatory effects. This class
of drugs has serious side effects at the gastrointestinal, renal and
cardiovascular, and this is due to the non-selective inhibition of cyclooxygenase isoforms.
Therefore, due to the current scenario related to the adverse effects caused by
NSAIDs, as well as the potential anti-inflammatory activity presented by AAs, the
This project aims to rationally obtain new therapeutic agents, with
potential anti-inflammatory activity related to selective inhibition of COX-2,
designed from saturated side chain anacardic acid linked to the system
1,2,3-triazole. This core maintains high stability under acid and basic hydrolysis, has the
ability to establish hydrogen bonds in the in vivo environment, in addition to performing
π-stacking interactions with relevant amino acid residues within the
enzymatic cavity due to its aromatic character triggering a series of
biological activities. The anti-inflammatory activity of the prepared AA derivatives
will be carried out by spectrophotometric assay, using the enzyme immunoassay kit
colorimetric, commercially obtained, which will evaluate the inhibitory capacity of
substances on the cyclooxygenase isoforms (COX-1 and COX-2), having the values
of IC 50 and selectivity indices determined and compared with the medicine
standard, Celecoxib

COMMITTEE MEMBERS:
Presidente - 3292567 - EDUARDO HILLMANN WANDERLIND
Interna - ***.742.388-** - AUREA ECHEVARRIA AZNAR NEVES LIMA - USP
Interno - 1058758 - MARCO EDILSON FREIRE DE LIMA
Externo ao Programa - 1674073 - BRUNO GUIMARAES MARINHO - UFRRJExterno ao Programa - 386960 - WELLINGTON DA SILVA CORTES - UFRRJ