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 Opportunities: Scholarships in Brazil - Master
• Start date: September 01, 2017
• End date: March 31, 2019
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Fernando Antonio Santos Coelho
• Grantee: Mariane Valéria Roldão
• Host 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.

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. Master's Dissertation - Universidade Estadual de Campinas (UNICAMP). Instituto de Química Campinas, SP.