Synthesis, and biological evaluation of new 1,3,4-thiadiazolium-2-phenylamine derivatives against Leishmania amazonensis promastigotes and amastigotes.
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.
da Silva
Edson F
EF
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal Rural de Rio de Janeiro, ICE, 23851-970 Seropédica (RJ), Brazil.
Canto-Cavalheiro
Marilene M
MM
Braz
Viviane R
VR
Cysne-Finkelstein
Léa
L
Leon
Leonor L
LL
Echevarria
Aurea
A
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
D000814:Aniline Compounds