Gustavo S. G. de Carvalho, Rafael M. P. Dias, Fernando R. Pavan, Clarice Q. F. Leite, Vania L. Silva, Claudio G. Diniz, Daniela T. S. de Paula, Elaine S. Coimbra, Pascal Retailleau and Adilson D. da Silva Pages 351 - 359 ( 9 )
This paper describes the synthesis and in vitro biological activities of imidazolidine and hexahydropyrimidine derivatives against bacteria (Escherichia coli, Staphylococcus aureus and Mycobacterium tuberculosis) and Leishmania protozoa. Out of sixteen heterocyclic derivatives tested, none were cytotoxic against mammalian cells. The compounds showed significant bacterial effects and leishmanicidal activity. Compounds 4a and 4c were active against S. aureus and E. coli, respectively. Compounds 3a-3f, 4h and 4i presented promising results against M. tuberculosis, with MIC values ranging from 12.5 to 25.0 μg/mL, comparable to the “first and second line” drugs used to treat tuberculosis. Compounds 4a, 4c and 4e were active against L major. Three of them were structurally characterized by single-crystal X-ray diffraction.
Synthesis, Cytotoxicity, Antibacterial, Antileishmanial, Biological Activities, Imidazolidine, Hexahydropyrimidine Derivatives, X-ray crystallography, Mycobacterium tuberculosis, heterocyclic compounds, E. coli
Departamento de Quimica, ICE, Universidade Federal de Juiz de Fora, 36036900, Juiz de Fora – MG, Brasil.