Can I read Studies Toward the Structural Optimization of Novel Thiazolylhydrazone-based Potent Antitrypanosomal Agents on EtoBox?

Studies Toward the Structural Optimization of Novel Thiazolylhydrazone-based Potent Antitrypanosomal Agents by Marcelo Zaldini Hernandes; Marcelo Montenegro Rabello; Ana Cristina Lima Leite; Marcos Veríssimo Oliveira Cardoso; Diogo Rodrigo Magalhaes Moreira; Dalci José Brondani; Carlos Alberto Simone; Luiza Campos Reis; Marina Assis Souza; Valéria Rego Alves Pereira; Rafaela Salgado Ferreira; James Hobson McKerrow is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Studies Toward the Structural Optimization of Novel Thiazolylhydrazone-based Potent Antitrypanosomal Agents about?

In previous studies, we identified promising anti-Trypanosoma cruzi cruzain inhibitors based on thiazolylhydrazones. To optimize this series, a number of medicinal chemistry directions were explored and new thiazolylhydrazones and thiosemicarbazones were thus synthesized. Potent cruzain inhibitors were identified, such as thiazolylhydrazones 3b and 3j, which exhibited IC 50 of 200-400 nM. Furthermore, molecular docking studies showed concordance with experimentally derived structure-activity relationships (SAR) data. In the course of this work, lead compounds exhibiting in vitro activity against both the epimastigote and trypomastigote forms of T. cruzi were identified and in vivo general toxicity analysis was subsequently performed. Novel SAR were documented, including the importance of the thiocarbonyl carbon attached to the thiazolyl ring and the direct comparison between thiosemicarbazones and thiazolylhydrazones.

Who reads Studies Toward the Structural Optimization of Novel Thiazolylhydrazone-based Potent Antitrypanosomal Agents?

Author

Marcelo Zaldini Hernandes; Marcelo Montenegro Rabello; Ana Cristina Lima Leite; Marcos Veríssimo Oliveira Cardoso; Diogo Rodrigo Magalhaes Moreira; Dalci José Brondani; Carlos Alberto Simone; Luiza Campos Reis; Marina Assis Souza; Valéria Rego Alves Pereira; Rafaela Salgado Ferreira; James Hobson McKerrow

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)