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Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives
- 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.
- 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
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Med Chem, Med Chem, 2013, 9 (3), pp.351-9, ResearcherID
- Accession number :
- edsair.doi.dedup.....821e7104ec946de029a2c08993f88edb