{"id":2130,"date":"2023-09-15T12:40:05","date_gmt":"2023-09-15T12:40:05","guid":{"rendered":"https:\/\/brazmedchem.org\/2023\/?post_type=palestra&#038;p=2130"},"modified":"2023-09-15T12:40:06","modified_gmt":"2023-09-15T12:40:06","slug":"cyclopeptides-containing-n-methyl-amino-acids-as-promising-antiplasmodial-agents","status":"publish","type":"palestra","link":"https:\/\/brazmedchem.org\/2023\/palestra\/cyclopeptides-containing-n-methyl-amino-acids-as-promising-antiplasmodial-agents\/","title":{"rendered":"Cyclopeptides Containing N-Methyl Amino Acids as Promising Antiplasmodial Agents."},"content":{"rendered":"\n<p>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.<\/p>\n\n\n\n<p>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.<\/p>\n\n\n\n<p>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 <em>P. falciparum<\/em> were performed. Several compounds showed subnanomolar or nanomolar EC<sub>50<\/sub> and high selectivity. Furthermore, two cyclopeptides have confirmed <em>in vivo<\/em> efficacy after oral administration. New investigations allowed us to obtain 4 polymeric nanoparticles containing active compounds that are being tested.<\/p>\n","protected":false},"template":"","class_list":["post-2130","palestra","type-palestra","status-publish","hentry"],"_links":{"self":[{"href":"https:\/\/brazmedchem.org\/2023\/wp-json\/wp\/v2\/palestra\/2130","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/brazmedchem.org\/2023\/wp-json\/wp\/v2\/palestra"}],"about":[{"href":"https:\/\/brazmedchem.org\/2023\/wp-json\/wp\/v2\/types\/palestra"}],"wp:attachment":[{"href":"https:\/\/brazmedchem.org\/2023\/wp-json\/wp\/v2\/media?parent=2130"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}