Banca de DEFESA: PAULO FERNANDO DA SILVA SANTOS JUNIOR

Uma banca de DEFESA de DOUTORADO foi cadastrada pelo programa.
STUDENT : PAULO FERNANDO DA SILVA SANTOS JUNIOR
DATE: 23/02/2022
TIME: 09:00
LOCAL: Google Meet
TITLE:
KEY WORDS:

2-aminothiophen-thiazolidines; Trypanosoma cruzi; Docking; Chagas disease; Amastigote forms.

PAGES: 244
BIG AREA: Ciências Exatas e da Terra
AREA: Química
SUBÁREA: Química Orgânica
SUMMARY:

Neglected diseases refer to a set of pathologies that affect around 1 billion individuals worldwide, who live in social exclusion and poverty, leading to a major global public health problem. Among the years 2000 and 2011, only 4% of all approved drugs (and 1% of new drugs) referred to the treatment of neglected diseases, which shows a profound lack of interest in research aimed at discovering new drugs and treatments for such pathologies. More than one hundred years after the discovery of Chagas disease, the therapeutic arsenal remains ineffective against the parasite, since it is based on the drugs Nifurtimox and Benznidazole. Such compounds have more than 50 years of use, coming to present several deleterious effects, in addition to parasitic resistance, making it necessary to discover new derivatives against this pathology. Thus, in a work recently reported by our research group, the derivative LQM83 was obtained, a molecular hybrid thiophene-thiazolidine, in which it showed potential inhibition against cruzaine, with IC₅₀ = 2.4 µM. Based on this, predicting to contribute directly to the improvement of the antichagasic therapeutic arsenal, this research comprises the synthesis of 7 series of seven compounds derived from LQM83 - thiophene-thiazolidine molecular hybrids. In this way, 8 intermediate compounds were obtained, in addition to 43 final compounds, with yields between 58-95% and 99% purity. Additionally, the structural characterization of these acids was carried out by means of Nuclear Magnetic Resonance of hydrogen (¹H) and carbon thirteen (¹³C), as well as PF. In addition, molecular Docking assays were performed in order to suggest possible interactions with the enzyme target in question, so that it was observed that the derivatives interact with the catalytic triad composed of Cys²⁵, Gly²³ and Gly⁶⁶.

BANKING MEMBERS:
Interno - 3182336 - EDEILDO FERREIRA DA SILVA JUNIOR
Interna - 1820117 - ISIS MARTINS FIGUEIREDO
Presidente - 1369387 - JOAO XAVIER DE ARAUJO JUNIOR
Externo à Instituição - JOHNNATAN DUARTE DE FREITAS - IFAL
Externa à Instituição - Lídia Moreira Lima - UFRJ
Interno - 1366289 - THIAGO MENDONCA DE AQUINO