Otro
Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives
Registro en:
Medicinal Chemistry, v. 9, n. 3, p. 351-359, 2013.
1573-4064
1875-6638
10.2174/1573406411309030005
WOS:000317910800004
2-s2.0-84877931409
Autor
De Carvalho, Gustavo S. G.
Dias, Rafael M. P.
Pavan, Fernando Rogério
Leite, Clarice Queico Fujimura
Silva, Vânia L.
Diniz, Cláudio G.
De Paula, Daniela T. S.
Coimbra, Elaine S.
Retailleau, Pascal
Da Silva, Adilson D.
Resumen
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. © 2013 Bentham Science Publishers. Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)