Banca de DEFESA: AFONSO SANTINE MAGALHÃES MESQUITA VELEZ

Uma banca de DEFESA de MESTRADO foi cadastrada pelo programa.
STUDENT : AFONSO SANTINE MAGALHÃES MESQUITA VELEZ
DATE: 27/05/2021
TIME: 09:00
LOCAL: Apresentação remota, via aplicativo
TITLE:

DESIGN AND SYNTHESIS OF NEW 1,2,4-TRIAZOL-3-THIOALKYL-NITROIMIDAZOLIC HYBRIDS WITH SELECTIVE TOXICITY AGAINST TRYPANOSOMA CRUZI AMASTIGOTES

KEY WORDS:

Piperine, Nitroimidazoles, Molecular hybridization

PAGES: 138
BIG AREA: Ciências Exatas e da Terra
AREA: Química
SUBÁREA: Química Orgânica
SPECIALTY: Síntese Orgânica
SUMMARY:

Chagas disease (CD) is one of the main neglected tropical diseases. CD is endemic in rural areas of developing countries in South and Central America, and to date it has no effective treatment. Facing the huge demand for the development of new compounds with therapeutic potential to treat neglected tropical diseases, this work aims to contribute to the study of the development of new drugs with potential antiparasitic activity. Our approach involved the application of the molecular hybridization strategy, using a 1,2,4-triazolic-3-thione derivative (with antiparasitic activity previously described by our group). This triazolic derivative was prepared from the natural amide piperine, the main chemical component of nuts of Piper nigrum, accessible natural product and easy isolation. The molecular planning carried out herein involved the hybridization of the triazolic derivative of piperine with different nitroimidazole cores (which stand out as important pharmacophores for the intended antiparasitic activity). The application of this molecular modification strategy, added to the other methodologies developed in this work, allowed the preparation of six new hybrids, which showed a very promising and selective activity against Trypanossoma cruzi amastigotes (Tulahuen strain, C2C4 LacZ).

 

BANKING MEMBERS:
Presidente - 1058758 - MARCO EDILSON FREIRE DE LIMA
Interno - 1700480 - ARTHUR EUGEN KUMMERLE
Externo à Instituição - GUSTAVO HENRIQUE GOULART TROSSINI - USP
Externo à Instituição - FERNANDO DE CARVALHO DA SILVA - UFF
Externo à Instituição - THIAGO MORENO LOPES E SOUZA - FIOCRUZ