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Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives

Authors :
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)
Brunet, Jocelyne
Source :
Med Chem, Med Chem, 2013, 9 (3), pp.351-9, ResearcherID
Publication Year :
2013
Publisher :
HAL CCSD, 2013.

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.

Details

Language :
English
Database :
OpenAIRE
Journal :
Med Chem, Med Chem, 2013, 9 (3), pp.351-9, ResearcherID
Accession number :
edsair.doi.dedup.....821e7104ec946de029a2c08993f88edb