Glória Serra

Full Professor at Pharmaceutical Chemistry Lab, Organic Chemistry Department, Universidad de la República (UdelaR). Head of Department of Organic chemistry since 2021.Her research focuses on the development of bioactive compounds for neglected tropical diseases and malaria, anti SARS-CoV2 agents and herbicides with activity against cyanobacteria. During the last ten years, her research also focused on the development and applications of synthetic strategies to obtain peptides and cyclopeptides. She was elected Director of PEDECIBA-Chemistry (2015-2018), Academic Coordinator (School of Chemistry, UdelaR) of AUGM (2001-2021) and guest editor of special collection “Organic and Supramolecular Chemistry in Latin America” of EurJOC journal.

Cyclopeptides Containing N-Methyl Amino Acids as Promising Antiplasmodial Agents.

The WHO 2022 Malaria Report, estimated 247 million cases and 619,000 deaths with the majority of infants under-five caused by malaria. Efforts to control the disease have decreased significantly the burden since 2000; however, this progression seems to be stalled during the last four years.

Based on the potential of macrocycles and on our previous work, we obtained tetra, penta and hexacyclopeptides, containing N-methyl amino acids to evaluate how N-methylation and/or the ring size affect the bioactivity of cyclopeptidic antimalarial compounds.

The syntheses of peptides by SPPS (Solid Phase Peptide Synthesis), the solution or on-resin macrocyclization using two methodologies,the activity and selectivity against the P. falciparum were performed. Several compounds showed subnanomolar or nanomolar EC50 and high selectivity. Furthermore, two cyclopeptides have confirmed in vivo efficacy after oral administration. New investigations allowed us to obtain 4 polymeric nanoparticles containing active compounds that are being tested.