title: Synthesis, and biological evaluation of new 1,3,4-thiadiazolium-2-phenylamine derivatives against Leishmania amazonensis promastigotes and amastigotes.
abstract: 1,3,4-thiadiazolium-2-aminide, which is a class of mesoionic compounds, were tested against promastigote and amastigote forms of Leishmania amazonensis. Parasites were assayed with or without the drugs in axenic media, using pentamidine isethionate as a reference drug. The very promising results showed us the most active compounds were the 4'- and 3'-methoxy derivatives against promastigote forms, while the highest activity against the amastigote forms was obtained with the 4'-fluor and 3'-bromo derivatives.
authors.affiliation: Departamento de Química, Instituto de Ciências Exatas, Universidade Federal Rural de Rio de Janeiro, ICE, 23851-970 Seropédica (RJ), Brazil.
authors.forename: Edson F
authors.initials: EF
authors.lastname: da Silva
authors.forename: Marilene M
authors.initials: MM
authors.lastname: Canto-Cavalheiro
authors.forename: Viviane R
authors.initials: VR
authors.lastname: Braz
authors.forename: Léa
authors.initials: L
authors.lastname: Cysne-Finkelstein
authors.forename: Leonor L
authors.initials: LL
authors.lastname: Leon
authors.forename: Aurea
authors.initials: A
authors.lastname: Echevarria
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D007892:Leishmania braziliensis / Q000187:drug effects* / Q000254:growth & development*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
chemical_list: D000814:Aniline Compounds