title: Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives.
abstract: 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.
authors.affiliation: Departamento de Quimica, Universidade Federal de Juiz de Fora, Juiz de Fora, Brasil.
authors.forename: Gustavo S G
authors.initials: GS
authors.lastname: de Carvalho
authors.forename: Rafael M P
authors.initials: RM
authors.lastname: Dias
authors.forename: Fernando R
authors.initials: FR
authors.lastname: Pavan
authors.forename: Clarice Q F
authors.initials: CQ
authors.lastname: Leite
authors.forename: Vania L
authors.initials: VL
authors.lastname: Silva
authors.forename: Claudio G
authors.initials: CG
authors.lastname: Diniz
authors.forename: Daniela T S
authors.initials: DT
authors.lastname: de Paula
authors.forename: Elaine S
authors.initials: ES
authors.lastname: Coimbra
authors.forename: Pascal
authors.initials: P
authors.lastname: Retailleau
authors.forename: Adilson D
authors.initials: AD
authors.lastname: da Silva
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D002478:Cells, Cultured; D018360:Crystallography, X-Ray; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007891:Leishmania / Q000187:drug effects*; D051379:Mice; D050296:Microbial Viability / Q000187:drug effects; D008958:Models, Molecular; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000977:Antiparasitic Agents; D048289:Imidazolidines; D011743:Pyrimidines