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Development of molecualar buiding blocks in the search of parasitic cysteine proteases

Grant number: 16/25870-6
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): May 01, 2017
Effective date (End): April 30, 2018
Field of knowledge:Health Sciences - Pharmacy
Principal researcher:Gustavo Henrique Goulart Trossini
Grantee:Carmem Castiñeira
Home Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Neglected diseases are so named because of the insufficient interest of the government and pharmaceutical industries coupled with ineffective therapies despite the great medical relevance, especially in underdeveloped and developing countries. Most prominently, it is faced with Chagas disease, considered extremely neglected, being this parasitic disease caused by the protozoa Trypanosoma cruzi. The identification and characterization of metabolic pathways essential for the survival of the parasite are fundamental bases for the rational planning of new chemotherapeutic agents. In this context, enzymes are targets of great interest as they play a key role in many diseases. As parasites, a class of enzymes that stands out, is the class of cysteine proteases, once, in addition to being found in abundance in protozoas, these are closely related to the life cycle and pathogenicity of parasites. In the context of drug planning, a current and interesting strategy lies in the development of building blocks for the usage in the synthesis of original and high quality prototypes. Such strategy is based on the fact that obtaining high quality of a prototype or high similarity of the prototype to a drug is provided by the originality of the synthesized molecules. Therefore, the present work aims at the application of several synthetic routes of building blocks of 5-aryl-substituted-2-amino-1,3,4-oxadiazoles derivatives to be used in the synthesis of bioactive compounds with biological activity against parasitic proteases. For the different molecules, obtained from enzymatic assays, their inhibition mechanisms will be determined as well as the potency and the affinity of such inhibitors against the parasitic cysteine proteases.

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