Banca de QUALIFICAÇÃO: LAMARK CARLOS I

Uma banca de QUALIFICAÇÃO de MESTRADO foi cadastrada pelo programa.
STUDENT : LAMARK CARLOS I
DATE: 28/04/2023
TIME: 09:00
LOCAL: Link de acesso para videoconferência: https://meet.google.com/cnk-abpa-yzr
TITLE:
SYNTHESIS OF NEW 1,2,3-TRIAZOLE INDOL DERIVATIVES WITH POTENTIAL ANTIMALARYAL ACTIVITY

KEY WORDS:
Malaria. Melatonin. Plasmodium Falciparum. 1,2,3-triazole-1,4-disubstituted. CuAAC. Tryptamine.

PAGES: 125
BIG AREA: Ciências da Saúde
AREA: Farmácia
SUMMARY:
Present in more than 90 countries, malaria is considered one of the most lethal infectious
diseases in the world. Caused by parasites of the genus Plasmodium, its vector is the female
Anopheles mosquito. The most recent data on the epidemiology of the disease released in 2022
by the World Health Organization (OMS) estimate that in 2021 there were about 247 million
cases of malaria worldwide, with more than 619,000 deaths. The search for new compounds
with antimalarial activity is urgent, as resistance to the classic drugs used in the treatment has
already been described in countries endemic to the disease. Melatonin is a hormone that has an
indole structure and plays a central role in controlling the replication of the parasite that causes
malaria and stabilizing the parasitemia. Blocking the pathway of this hormone may contribute
to the discovery of new antimalarial drugs. Specific therapy options for this disease also depend
on the species of parasite causing the infection. Thus, it is important to discover new substances
that can be used in the treatment of this disease. This work aimed to prepare derivatives of
melatonin that could exhibit antimalarial activity on the parasite's cell cycle, inhibiting the
growth or causing the death of Plasmodium falciparum. Several unpublished molecules
containing in their structure, 1,2,3-triazole heterocyclic rings and benzene ring with different
substituents were planned and synthesized in this work. In the synthesis step, the melatonin
precursor was subjected to a hydrolysis reaction to form the free amine group. Subsequently,
this intermediate was treated with 4-nitrobenzenesulfonyl chloride, propargyl bromide and
different aromatic azidocompounds for the formation of the respective products containing in
their structure the desired indole and 1,2,3-triazole-1,4-disubstituted nuclei through the CuAAC
click chemistry reaction catalyzed by copper(I). Tryptamine, a congener of melatonin, will also
be used as a precursor in the formation of triazole compounds.Tryptamine, a congener of
melatonin, will also be used as a precursor in the formation of triazole compounds. The
characterization of the products was carried out by spectroscopic techniques of infrared and
nuclear magnetic resonance of 13C and 1H isotopes. The compounds obtained will be sent for
antimalarial evaluation by determination of parasitemia and IC50.

COMMITTEE MEMBERS:
Externa à Instituição - LUCIANA DA CUNHA COSTA - UERJ
Presidente - 1492900 - CICERO FLAVIO SOARES ARAGAO
Externo ao Programa - 1803692 - FABRICIO GAVA MENEZES - null
Notícia cadastrada em: 17/04/2023 10:21
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