1. Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives
- Author
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Vânia Lúcia da Silva, Pascal Retailleau, Gustavo S.G. de Carvalho, Fernando Rogério Pavan, Rafael M. P. Dias, Cláudio Galuppo Diniz, Adilson David da Silva, Clarice Queico Fujimura Leite, Elaine Soares Coimbra, Daniela T. S. de Paula, Institut de Chimie des Substances Naturelles (ICSN), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), and Brunet, Jocelyne
- Subjects
Models, Molecular ,Stereochemistry ,Biology ,Crystallography, X-Ray ,Imidazolidines ,010402 general chemistry ,medicine.disease_cause ,01 natural sciences ,Mycobacterium tuberculosis ,Mice ,chemistry.chemical_compound ,Imidazolidine ,Drug Discovery ,medicine ,Animals ,Humans ,Cells, Cultured ,Leishmania ,chemistry.chemical_classification ,Antiinfective agent ,Microbial Viability ,Antiparasitic Agents ,Bacteria ,Molecular Structure ,010405 organic chemistry ,[CHIM.ORGA]Chemical Sciences/Organic chemistry ,Biological activity ,[CHIM.ORGA] Chemical Sciences/Organic chemistry ,biology.organism_classification ,Antiparasitic agent ,Anti-Bacterial Agents ,0104 chemical sciences ,3. Good health ,Pyrimidines ,chemistry ,Heterocyclic compound ,Staphylococcus aureus ,Antibacterial activity - Abstract
International audience; 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.
- Published
- 2013