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New synthetic approach for the preparation of non-steroidal anti-inflammatory drugs, selective COX-2 inhibitors: study of mechanisms of anti-inflammatory action

Grant number: 17/08229-8
Support type:Scholarships in Brazil - Master
Effective date (Start): September 01, 2017
Effective date (End): March 31, 2019
Field of knowledge:Health Sciences - Pharmacy
Principal researcher:Fernando Antonio Santos Coelho
Grantee:Mariane Valéria Roldão
Home Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil

Abstract

This Master's degree research project has as its main target the proposal of a new synthetic approach for the preparation of a class of anti-inflammatory substances, which were previously synthesized in our laboratory. Based on Morita-Baylis-Hillman adducts, we developed a synthetic strategy that allowed the synthesis of a small series of compounds presenting a very promising anti-inflammatory activity (fully demonstrated by in vitro and in vivo essays). However, the established sequence is long (8 steps) and used as key-step a coupling reaction mediated by rhodium, which is highly sensitive to the nature of the substrate. Due to the excellent anti-inflammatory profile of these compounds, we therefore decided to re-visit this work aiming at proposing a new, general and simple synthetic strategy, which will allow not only the synthesis of a library of compounds, but also a more detailed study of the biological mechanism of action of these compounds.

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Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
ROLDÃO, Mariane Valéria. Diastereoselective synthesis of a new dissubstitued cyclopentenones series with potential anti-inflammatory activity. 2019. 360 f. Master's Dissertation - Universidade Estadual de Campinas (UNICAMP). Instituto de Química.

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