Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives
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Data
2013-05-01
Autores
De Carvalho, Gustavo S. G.
Dias, Rafael M. P.
Pavan, Fernando Rogério [UNESP]
Leite, Clarice Queico Fujimura [UNESP]
Silva, Vânia L.
Diniz, Cláudio G.
De Paula, Daniela T. S.
Coimbra, Elaine S.
Retailleau, Pascal
Da Silva, Adilson D.
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Resumo
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.
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Palavras-chave
Antibacterial, Antileishmanial, Biological activities, Cytotoxicity, Hexahydropyrimidine derivatives, Imidazolidine, Synthesis, X-ray crystallography, antiinfective agent, antileishmanial agent, heterocyclic compound, hexahydropyrimidine derivative, imidazolidine derivative, unclassified drug, animal cell, antibacterial activity, biological activity, controlled study, crystal structure, cytotoxicity, drug structure, drug synthesis, Escherichia coli, in vitro study, Leishmania, Leishmania major, minimum inhibitory concentration, mouse, Mycobacterium tuberculosis, nonhuman, priority journal, Staphylococcus aureus, X ray crystallography, X ray diffraction, Animals, Anti-Bacterial Agents, Antiparasitic Agents, Bacteria, Cells, Cultured, Crystallography, X-Ray, Humans, Imidazolidines, Mice, Microbial Viability, Models, Molecular, Molecular Structure, Pyrimidines
Como citar
Medicinal Chemistry, v. 9, n. 3, p. 351-359, 2013.